Dactolisib | ATM/ATR | mTOR | PI3K | AmBeed-信号通路专用抑制剂

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Dactolisib 99%+

货号：A224243

Dactolisib（BEZ235）是一种口服活性的双重抑制剂，对pan-class I PI3K和mTOR激酶的IC50值分别为4 nM、5 nM、7 nM和75 nM，对mTOR的IC50值为20.7 nM。Dactolisib抑制mTORC1和mTORC2。

Dactolisib 化学结构
CAS号：915019-65-7

Dactolisib 3D分子结构
CAS号：915019-65-7

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Dactolisib 纯度/质量文件产品仅供科研

货号：A224243 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024. Ambeed. [ A288696 ]; • JMC, 2024. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

mTOR 亚型比较
PI3K 亚型比较
ATM/ATR 亚型比较

产品名称	mTOR ↓ ↑	mTORC1 ↓ ↑	mTORC2 ↓ ↑	其他靶点	纯度
AZD-8055	++++ mTOR (truncated), IC50: 0.13 nM mTOR (full length), IC50: 0.8 nM				99%+
Gedatolisib	++++ mTOR, IC50: 1.6 nM				99%+
GSK1059615	++ mTOR, IC50: 12 nM				98%
Vistusertib	+++ mTOR, IC50: 2.8 nM				99%+
Torin 1	+++ mTOR, IC50: 4.32 nM	+++ mTORC1, IC50: 2 nM	++ mTORC2, IC50: 10 nM	DNA-PK	99%+
Dactolisib	+++ mTOR (p70S6K), IC50: 6 nM				99%+
PI-103	+ mTOR, IC50: 30 nM				99%+
WAY-600	++ mTOR, IC50: 9 nM				99%
Voxtalisib	+ mTOR, IC50: 157 nM				99%+
PF-04691502	++ mTOR, Ki: 16 nM				99%+
Onatasertib	++ mTOR, IC50: 16 nM			DNA-PK	99%+
Chrysophanol	✔			EGFR	98%
Samotolisib	✔			DNA-PK	99%+
Torkinib	+++ mTOR, IC50: 8 nM			DNA-PK,PDGFR	99%+
Everolimus					99%+
WYE-354	+++ mTOR, IC50: 5 nM				99%+
Tacrolimus	✔				98%
PP121	++ mTOR, IC50: 13 nM			VEGFR,PDGFR	99%+
Torin 2	++++ mTOR, IC50: 0.25 nM			DNA-PK	99%+
Rapamycin	++++ mTOR, IC50: ~0.1 nM				98%
GDC-0349	+++ mTOR, Ki: 3.8 nM				98%
XL388	++ mTOR, IC50: 9.9 nM	+++ mTORC1, IC50: 8 nM	+ mTORC2, IC50: 166 nM		99%+
WYE-687	+++ mTOR, IC50: 7 nM				98+%
Apitolisib	+ mTOR, Ki app: 17 nM				99%+
WYE-132	++++ mTOR, IC50: 0.19 nM				99%+
Sapanisertib	++++ mTOR, Ki: 1.4 nM				99%+
BGT226 maleate	✔				99%+
ETP-46464	++++ mTOR, IC50: 0.6 nM			DNA-PK	99%+
PI3K-IN-1	+ mTOR, IC50: 157 nM				99%+
Zotarolimus	+++ FKBP-12, IC50: 2.8 nM				99+%
OSI-027	+++ mTOR, IC50: 4 nM	+ mTORC1, IC50: 22 nM	+ mTORC2, IC50: 65 nM		99%+
Ridaforolimus	++++ mTOR, IC50: 0.2 nM				99%+
Temsirolimus	+ mTOR, IC50: 1.76 μM				99%
CZ415	++ mTOR, pIC50: 8.07				99%+
SF2523	+ mTOR, IC50: 280 nM			DNA-PK	99%+
KU-0063794		++ mTORC1, IC50: ~10 nM	++ mTORC2, IC50: ~10 nM		99%+
Omipalisib		++++ mTORC1, Ki: 0.18 nM	++++ mTORC2, Ki: 0.3 nM		99%+
Palomid 529		✔			99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	C2β ↓ ↑	p110α ↓ ↑	p110β ↓ ↑	p110γ ↓ ↑	p110δ ↓ ↑	PI3K ↓ ↑	Vps34 ↓ ↑	其他靶点	纯度
A66	+ C2β, IC50: 462 nM	++ p110α, IC50: 32 nM							99%+
Taselisib	+ C2β, IC50: 292 nM	++++ PI3Kα, Ki: 0.29 nM	+++ PI3Kβ, Ki: 9.1 nM	++++ PI3Kγ, Ki: 0.97 nM	++++ PI3Kδ, Ki: 0.12 nM		+ hVps34, IC50: 374 nM		99%+
Gedatolisib		++++ PI3Kα, IC50: 0.4 nM		+++ PI3Kγ, IC50: 5.4 nM				mTOR	99%+
HS-173		++++ PI3Kα , IC50: 0.8 nM							99%+
Serabelisib		+++ PI3Kα, IC50: 21 nM							99%+
GNE-477		++++ PI3Kα, IC50: 4 nM						mTOR	99%+
YM-201636		+ p110α, IC50: 3.3 μM						PIKfyve	99%+
AS-252424		+ PI3Kα, IC50: 935 nM		++ PI3Kγ, IC50: 33 nM					99%
Alpelisib		+++ PI3Kα, IC50: 5 nM							99%+
AS-604850		+ PI3Kα, IC50: 4.5 μM		+ PI3Kγ, IC50: 0.25 μM					99%+
SF2523		++ PI3Kα, IC50: 34 nM		++ PI3Kγ, IC50: 158 nM				DNA-PK,mTOR	99%+
Inavolisib		++++ PI3K alpha, IC50: 0.038 nM							99%+
Bimiralisib		++++ PI3Kα, Kd: 1.5 nM	+++ PI3Kβ, Kd: 11 nM	++ PI3Kγ, Kd: 25 nM	++ PI3Kδ, Kd: 25 nM			mTOR	99%+
GSK1059615		++++ PI3Kα, IC50: 0.4 nM	++++ PI3Kβ, IC50: 0.6 nM	+++ PI3Kγ, IC50: 5 nM	++++ PI3Kδ, IC50: 2 nM			mTOR	98%
GSK2636771			✔						99%+
Fimepinostat		+++ PI3Kα, IC50: 19 nM	++ PI3Kβ, IC50: 54 nM		++ PI3Kδ, IC50: 39 nM				99%+
VS-5584		++++ PI3Kα, IC50: 2.6 nM	+++ PI3Kβ, IC50: 21 nM	++++ PI3Kγ, IC50: 3.0 nM	++++ PI3Kδ, IC50: 2.7 nM			mTOR	99%
Dactolisib		++++ p110α1, IC50: 4 nM	++ p110β, IC50: 75 nM	+++ p110γ, IC50: 5 nM	+++ p110δ, IC50: 7 nM				99%+
PI-103		++++ p110α, IC50: 2 nM	++++ p110β, IC50: 3 nM	+++ p110γ, IC50: 15 nM	++++ p110δ, IC50: 3 nM			DNA-PK,mTOR	99%+
PI-3065			+ p110β, IC50: 1078 nM		+++ p110δ, IC50: 15 nM				99%+
Voxtalisib		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	99%+
AZD-8835		+++ PI3Kα, IC50: 6.2 nM	+ PI3Kβ, IC50: 431 nM	++ PI3Kγ, IC50: 90 nM	+++ PI3Kδ, IC50: 5.7 nM				99%+
Pilaralisib analogue		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 36 nM	+++ PI3Kγ, IC50: 23 nM	++ PI3Kδ, IC50: 36 nM				99%+
ZSTK474		+++ PI3Kα, IC50: 16 nM	++ PI3Kβ, IC50: 44 nM	++ PI3Kγ, IC50: 49 nM	+++ PI3Kδ, IC50: 4.6 nM	++ PI3K, IC50: 37 nM			99%+
AS-605240		++ PI3Kα, IC50: 60 nM	+ PI3Kβ, IC50: 270 nM	+++ PI3Kγ, IC50: 8 nM	+ PI3Kδ, IC50: 300 nM				99%+
TGX-221			+++ p110β, IC50: 5 nM		++ p110δ, IC50: 0.1 μM				99%+
PF-04691502		++++ PI3Kα, Ki: 1.8 nM	++++ PI3Kβ, Ki: 2.1 nM	++++ PI3Kγ, Ki: 1.9 nM	++++ PI3Kδ, Ki: 1.6 nM			mTOR	99%+
GDC-0084		++++ PI3Kα, Ki app: 2 nM	++ PI3Kβ, Ki app: 46 nM	+++ PI3Kγ, Ki app: 10 nM	++++ PI3Kδ, Ki app: 3 nM			mTOR	99%+
Buparlisib		++ p110α, IC50: 52 nM	+ p110β, IC50: 166 nM	+ p110γ, IC50: 262 nM	++ p110δ, IC50: 116 nM		+ Vps34, IC50: 2.4 μM	mTOR	98%
LY294002		+ p110α, IC50: 0.5 μM	+ p110β, IC50: 0.97 μM		+ p110δ, IC50: 0.57 μM			DNA-PK	99%+
AZD 6482		+ PI3Kα, IC50: 870 nM	+++ PI3Kβ, IC50: 10 nM		++ PI3Kδ, IC50: 80 nM			DNA-PK	99%+
Pictilisib		++++ p110α, IC50: 3 nM	++ p110β, IC50: 33 nM	++ p110γ, IC50: 75 nM	++++ p110δ, IC50: 3 nM			mTOR	99%+
PKI-402		++++ PI3Kα, IC50: 2 nM	+++ PI3Kβ, IC50: 7 nM	+++ PI3Kγ, IC50: 16 nM	+++ PI3Kδ, IC50: 14 nM			mTOR	99+%
Copanlisib		++++ PI3Kα, IC50: 0.5 nM	++++ PI3Kβ, IC50: 3.7 nM	+++ PI3Kγ, IC50: 6.4 nM	++++ PI3Kδ, IC50: 0.7 nM				99%+
Omipalisib		++++ p110α, Ki: 0.019 nM	++++ p110β, Ki: 0.13 nM	++++ p110γ, Ki: 0.06 nM	++++ p110δ, Ki: 0.024 nM				99%+
Izorlisib		+++ PI3Kα, IC50: 14 nM	++ PI3Kβ, IC50: 0.12 μM	++ PI3Kγ, IC50: 36 nM	+ PI3Kδ, IC50: 0.50 μM				99%+
AZD8186		++ PI3Kα, IC50: 35 nM	++++ PI3Kβ, IC50: 4 nM		+++ PI3Kδ, IC50: 12 nM				99%+
KU-0060648		++++ PI3Kα, IC50: 4 nM	++++ PI3Kβ, IC50: 0.5 nM	+ PI3Kγ, IC50: 0.59 μM	++++ PI3Kδ, IC50: 0.1 nM			DNA-PK	99%
Apitolisib		+++ p110α, IC50: 5 nM	++ p110β, IC50: 27 nM	+++ p110γ, IC50: 14 nM	+++ p110δ, IC50: 7 nM			mTOR	99%+
CZC24832			+ PI3Kβ, IC50: 1.1 μM	++ PI3Kγ, IC50: 27 nM					99%+
BGT226 maleate		++++ PI3Kα, IC50: 4 nM	++ PI3Kβ, IC50: 63 nM	++ PI3Kγ, IC50: 38 nM				mTOR	99%+
TG 100713		++ PI3Kα, IC50: 165 nM	+ PI3Kβ, IC50: 215 nM	++ PI3Kγ, IC50: 50 nM	+++ PI3Kδ, IC50: 24 nM				99%+
PI3K-IN-1		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	99%+
TG100-115		+ PI3Kα, IC50: 1.3 μM	+ PI3Kβ, IC50: 1.2 μM	++ PI3Kγ, IC50: 83 nM	+ PI3Kδ, IC50: 235 nM				99%+
PIK-90		+++ PI3Kα, IC50: 11 nM	+ PI3Kβ, IC50: 350 nM	+++ PI3Kγ, IC50: 18 nM	++ PI3Kδ, IC50: 58 nM				99%+
PIK-294			+ p110β, IC50: 490 nM	++ p110γ, IC50: 160 nM	+++ p110δ, IC50: 10 nM				99%+
Duvelisib			++++ PI3Kβ, Ki: 1564 pM	++ PI3Kγ, Ki: 243 pM	++++ PI3Kδ, Ki: 23 pM				99%+
GDC-0326		++++ PI3Kα, Ki: 0.2 nM	++ PI3Kβ, Ki: 26.6 nM	+++ PI3Kγ, Ki: 10.2 nM	++++ PI3Kδ, Ki: 4 nM				98%
Quercetin Dihydrate			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM				98%+
Quercetin			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM			Src,Sirtuin,PKC	97%
Leniolisib		+ PI3Kα, IC50: 0.244 μM	+ PI3Kβ, IC50: 0.424 μM	+ PI3Kγ, IC50: 2.23 μM	+++ PI3Kδ, IC50: 0.011 μM			DNA-PK	99%+
PIK-108			✔						99%+
Eganelisib				+++ PI3Kγ, IC50: 16 nM					99%+
CAY10505				✔					99%+
IPI-3063					++++ p110δ, IC50: 2.5 nM				99%
Nemiralisib					++++ PI3Kδ, pKi: 9.9				99%+
PF-4989216		++++ p110α, IC50: 2 nM		++ p110γ, IC50: 65 nM	++++ p110δ, IC50: 1 nM				99%+
PIK-75 HCl		+++ p110α, IC50: 5.8 nM		++ p110γ, IC50: 76 nM	+ p110δ, IC50: 0.51 μM			DNA-PK	99%+
Tenalisib				++ PI3Kγ, IC50: 33.2 nM	++ PI3Kδ, IC50: 24.5 nM				98%+
Acalisib					+++ p110δ, IC50: 14 nM				99%+
Umbralisib					+++ PI3Kδ, IC50: 22.2 nM				99%+
AMG319				+ PI3Kγ, IC50: 850 nM	+++ PI3Kδ, IC50: 18 nM				99%
IC-87114				+ PI3Kγ, IC50: 29 μM	+ PI3Kδ, IC50: 0.5 μM				99%+
Idelalisib				++ p110γ, IC50: 89 nM	++++ p110δ, IC50: 2.5 nM				98%
PIK-293				+ p110γ, IC50: 10 μM	+ p110δ, IC50: 0.24 μM				99%+
Vps34-PIK-III					+ PI3Kδ, IC50: 1.2μM		+++ Vps34, IC50: 0.018μM		99%+
GSK2292767					✔				99+%
Seletalisib				+ PI3Kγ, IC50: 282 nM	+++ PI3Kδ, IC50: 12 nM				99%+
P110δ-IN-1					++++ P110δ, IC50: 0.6 nM				99%+
PI3Kδ-IN-5					++++ PI3Kδ, IC50: 0.9 nM				99%+
SRX3207		+ PI3K alpha, IC50: 244 nM		+ PI3K gamma, IC50: 9790 nM	+ PI3K delta, IC50: 388 nM			Syk	98%
Parsaclisib HCl					++++ PI3Kδ, IC50: 1 nM				98%
IHMT-PI3Kδ-372					+++ PI3Kδ, IC50: 14 nM				98%
Trigonelline						✔		Akt	99%+
Wortmannin						++++ PI3K, IC50: 3 nM		MLCK,DNA-PK	99%+
Samotolisib						✔		DNA-PK	99%+
GNE-317						✔			99%+
Oroxin B						✔		Akt,PTEN	99%+
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	99%+
Deguelin						✔		Akt	99%+
Ailanthone						✔		CDK,Akt,ATM/ATR	98%
Resibufogenin						✔		ROS	98%
KU-57788						+ PI3K, IC50: 5 μM		DNA-PK,mTOR	99%+
Cinobufagine						✔		Akt	98%
α-Linolenic acid						✔			97% GC
MTX-211						✔		EGFR	99%+
PI3K/mTOR Inhibitor-2						++++ PI3K, IC50: 3.4 nM		mTOR	99%+
SPP-86						✔			99%+
(E)-Akt inhibitor-IV						✔			98%
Vps34-IN-1							++ Vps34, IC50: 25 nM		98%
SAR405							++++ Vps34, IC50: 1.2 nM		99%+
3-Methyladenine				+ PI3Kγ, IC50: 60 μM			+ Vps34, IC50: 25 μM	Autophagy	98%
Vps34-IN-4							+++ VPS34, IC50: 15 nM		99%+
Autophinib							+++ Vps34, IC50: 19 nM	Autophagy	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	ATM ↓ ↑	ATR ↓ ↑	其他靶点	纯度
Wortmannin	++ ATM, IC50: 150 nM		MLCK,DNA-PK,PI3K	99%+
CP-466722	+ ATM, IC50: 410 nM			99%+
Torin 2	++ ATM, EC50: 28 nM	++ ATR, EC50: 35 nM	mTOR,DNA-PK	99%+
KU-55933	+++ ATM, IC50: 12.9 nM			99%+
ETP-46464	+ ATM, IC50: 545 nM	+++ ATR, IC50: 14 nM	mTOR,DNA-PK	99%+
CGK733	++ ATM, IC50: 200 nM	++ ATR, IC50: 200 nM		99%+
AZD0156	✔			99%+
Dactolisib		+++ ATR, IC50: 21 nM		99%+
Ceralasertib		++++ ATR, IC50: 1 nM		99%+
Berzosertib		+++ ATR, IC50: 19 nM		99%+
VE-821		+++ ATR, Ki: 13 nM		99%+
AZ20		++++ ATR, IC50: 5 nM	mTOR	99%+
Schizandrin B		+ ATR, IC50: 7.25 μM	P-gp	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Dactolisib 生物活性

靶点	p110γ p110γ, IC50:5 nM p110β p110β, IC50:75 nM p110α p110α1, IC50:4 nM p110δ p110δ, IC50:7 nM
描述	Aberrant activation of phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin inhibitor (mTOR) signaling pathway promotes the proliferation and survival of various human tumor cells. BEZ235 is a ATP competitive inhibitor of PI3K that inhibits the kinase activity of Class I PI3K p110α/β/δ/γ with IC50 of 4 nM, 75 nM, 7 nM, and 5 nM, respectively. In U87MG glioblastoma cells, the exposure of 0.1 - 1000 nM BEZ235 for 30 min reduced S473P-Akt and T308P-Akt levels in a dose-dependent manner, and the 50% reduction occurred at the doses of 8 nM and 30 nM, respectively. In NWT21 cells, pretreatment of 250 nM BEZ235 reduced insulin-like growth factor-I-induced S473P-Akt level. In starved HT-29 cells, BEZ235 at 250 nM efficiently inhibited interleukin-4-induced S473P-Akt level. The phosphorylation level of mTOR activated kinase p70^S6K was significantly reduced by 250 nM BEZ235 in U87MG cells after 30 min incubation. The S235/S236P-RPS6 level in TSC1-null MEF cells was decreased by BEZ235 with an IC50 of 6.5 nM. The addition of BEZ235 (5 - 500 nM) dose-dependently downregulated mTORC1 and mTORC2 activities in IgG-Sepharose pull-downs of HeLa cells. BEZ235 also showed inhibitory effect on cell proliferation. The G_{1_{population of PC3M cells was increased from 66.4% to 74.1% and 92.3% after the treatment with 10 nM and 50 nM BEZ235, respectively. In U87MG tumor-bearing mice, treatment of BEZ235 (25 – 45 mg/kg/d, once daily) for 20 days inhibited tumor growth and reduced S473P-Akt levels in the tumor at a dose-dependent manner^[3].}}
作用机制	BEZ235 inhibits PI3K via binding to its ATP-binding cleft^[3].

Dactolisib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A3-KAW		Growth Inhibition Assay		IC50=28.64 nM	SANGER
A427		Growth Inhibition Assay		IC50=182.57 nM	SANGER
A431		Growth Inhibition Assay		IC50=89.97 nM	SANGER
A498		Growth Inhibition Assay		IC50=75.15 nM	SANGER

Dactolisib 动物研究

Dose	Mice^[3] (p.o.): min = 1 mg/kg, max = 50 mg/kg
Administration	p.o.

Dactolisib 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01285466	Metastatic or Locally Advanced... 展开 >> Solid Tumors 收起 <<	Phase 1	Completed	-	Belgium ... 展开 >> Novartis Investigative Site Bruxelles, Belgium, 1000 Novartis Investigative Site Bruxelles, Belgium, 1200 Novartis Investigative Site Wilrijk, Belgium, 2610 Germany Novartis Investigative Site Essen, Germany, 45147 Novartis Investigative Site Köln, Germany, 50937 Netherlands Novartis Investigative Site Amsterdam, Netherlands, 1066 CX Spain Novartis Investigative Site Sevilla, Andalucia, Spain, 41013 Novartis Investigative Site Barcelona, Catalunya, Spain, 08035 Switzerland Novartis Investigative Site Chur, Switzerland, 7000 Novartis Investigative Site St. Gallen, Switzerland, 9007 收起 <<
NCT02430363	Glioblastoma	Phase 1 Phase 2	Unknown	June 2018	United States, Massachusetts ... 展开 >> Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Texas M D Anderson Cancer Center Houston, Texas, United States, 77030 Belgium UCL- Cliniques Universitaires Saint Luc Brussels, Belgium Germany St Johannes Hospital Duisburg, Germany, 47166 Italy Spedali Civili di Brescia Brescia, Italy IRCCS San Raffaele Milan, Italy Poland Lower-Silesian Oncology Centre Wroclaw, Lower-Silesian, Poland, 53413 Russian Federation Pavlov State Medical University St. Petersburg, Russian Federation, 197089 Spain Hospital Universitario Germans Trias I Pujol Barcelona,, Spain Switzerland Universitätsklinik für Frauenheilkunde Bern, Switzerland Ukraine Regional Cancer Center Dnepropetrovsk, Ukraine, 49000 National Institute of Cancer Kiev, Ukraine, 03035 United Kingdom Royal Victoria Hospital Belfast, Ulster, United Kingdom, BT12 6BA 收起 <<
NCT01508104	Cancer	Phase 1	Terminated(funding)	-	United States, Ohio ... 展开 >> University of Cincinnati Cincinnati, Ohio, United States, 45267-0502 收起 <<

Dactolisib 参考文献

[1]7(7):1851-63.

Dactolisib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.06mL

21.30mL

4.26mL

2.13mL

Dactolisib 技术信息

CAS号	915019-65-7
分子式	C₃₀H₂₃N₅O
分子量	469.536

别名
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 6 mg/mL(12.78 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

DMF: 2 mg/mL(4.26 mM)，配合低频超声助溶

动物实验配方

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摩尔计算器

计算溶液所需的质量，体积或浓度。 Ambeed 摩尔浓度计算器基于以下方程式：

浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

浓度

体积

分子量

质量

*在制备母液时，请始终参考产品标签或 MSDS / COA（在产品页面可下载）上所显示的对应批次产品的分子量。

靶点

靶点	数值

p110γ	p110γ, IC50:5 nM
p110β	p110β, IC50:75 nM
p110α	p110α1, IC50:4 nM
p110δ	p110δ, IC50:7 nM
mTOR	mTOR (p70S6K), IC50:6 nM
ATR	ATR, IC50:21 nM

总药量计算器

动物实验：给药剂量 mg/kg 动物体重 g 动物数量只每天给药次给药天

需要的总药量： mg

工作液计算器

动物实验：给药剂量 mg/kg 动物体重 g 给药体积 μL

您需要配制的工作液浓度为：mg/mL

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

A3-KAW		Growth Inhibition Assay		IC50=28.64 nM	SANGER
A427		Growth Inhibition Assay		IC50=182.57 nM	SANGER
A431		Growth Inhibition Assay		IC50=89.97 nM	SANGER
A498		Growth Inhibition Assay		IC50=75.15 nM	SANGER
A4-Fuk		Growth Inhibition Assay		IC50=46.52 nM	SANGER
A549	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.07 M	22336246
A549		Growth Inhibition Assay		IC50=10.14 nM	SANGER
A673		Growth Inhibition Assay		IC50=20.5507 μM	SANGER
A704		Growth Inhibition Assay		IC50=55.59 nM	SANGER
ABC-1		Growth Inhibition Assay		IC50=420.45 nM	SANGER
ACHN	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.95 M	22336246
ACHN		Growth Inhibition Assay		IC50=356.71 nM	SANGER
AGS		Growth Inhibition Assay		IC50=48.77 nM	SANGER
ALL-PO		Growth Inhibition Assay		IC50=415.69 nM	SANGER
AM-38		Growth Inhibition Assay		IC50=69.31 nM	SANGER
AN3-CA		Growth Inhibition Assay		IC50=5.56 nM	SANGER
AsPC-1		Growth Inhibition Assay		IC50=30.2 nM	SANGER
ATN-1		Growth Inhibition Assay		IC50=73.87 nM	SANGER
AU565		Growth Inhibition Assay		IC50=212.82 nM	SANGER
BALL-1		Growth Inhibition Assay		IC50=8.50409 μM	SANGER
BB30-HNC		Growth Inhibition Assay		IC50=130.78 nM	SANGER
BB49-HNC		Growth Inhibition Assay		IC50=173.81 nM	SANGER
BB65-RCC		Growth Inhibition Assay		IC50=12.72 nM	SANGER
BCPAP		Growth Inhibition Assay		IC50=18.65 nM	SANGER
BE-13		Growth Inhibition Assay		IC50=31.82 nM	SANGER
Becker		Growth Inhibition Assay		IC50=34.21 nM	SANGER
BEN		Growth Inhibition Assay		IC50=31.63 nM	SANGER
BFTC-905		Growth Inhibition Assay		IC50=60.65 nM	SANGER
BFTC-909		Growth Inhibition Assay		IC50=3.71 nM	SANGER
BHT-101		Growth Inhibition Assay		IC50=30.05 nM	SANGER
BHY		Growth Inhibition Assay		IC50=42.72 nM	SANGER
BPH-1		Growth Inhibition Assay		IC50=4.76 nM	SANGER
BSY1	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.48 M	22336246
BT-20		Growth Inhibition Assay		IC50=112.01 nM	SANGER
BT-474		Growth Inhibition Assay		IC50=235.73 nM	SANGER
BT-549		Growth Inhibition Assay		IC50=118.95 nM	SANGER
BV-173		Growth Inhibition Assay		IC50=23.87 nM	SANGER
BxPC-3		Growth Inhibition Assay		IC50=81.46 nM	SANGER
C2BBe1		Growth Inhibition Assay		IC50=75.03 nM	SANGER
C32		Growth Inhibition Assay		IC50=53.83 nM	SANGER
C-33-A		Growth Inhibition Assay		IC50=135.97 nM	SANGER
C3A		Growth Inhibition Assay		IC50=9.88394 μM	SANGER
C8166		Growth Inhibition Assay		IC50=2.63392 μM	SANGER
Ca9-22		Growth Inhibition Assay		IC50=33.55 nM	SANGER
CAKI-1		Growth Inhibition Assay		IC50=36.43 nM	SANGER
CAL-120		Growth Inhibition Assay		IC50=34.72 nM	SANGER
CAL-12T		Growth Inhibition Assay		IC50=38.6 nM	SANGER
CAL-27		Growth Inhibition Assay		IC50=217.05 nM	SANGER
CAL-33		Growth Inhibition Assay		IC50=85.08 nM	SANGER
CAL-39		Growth Inhibition Assay		IC50=37.9 nM	SANGER
CAL-51		Growth Inhibition Assay		IC50=23.89 nM	SANGER
CAL-54		Growth Inhibition Assay		IC50=238.49 nM	SANGER
CAL-62		Growth Inhibition Assay		IC50=36.86 nM	SANGER
CAL-72		Growth Inhibition Assay		IC50=293.19 nM	SANGER
CAL-85-1		Growth Inhibition Assay		IC50=92.48 nM	SANGER
Calu-3		Growth Inhibition Assay		IC50=71.98 nM	SANGER
Calu-6		Growth Inhibition Assay		IC50=3.1997 μM	SANGER
CAMA-1		Growth Inhibition Assay		IC50=9.8 nM	SANGER
CAN		Growth Inhibition Assay		IC50=81.84 nM	SANGER
CAPAN-1		Growth Inhibition Assay		IC50=7.62233 μM	SANGER
Capan-2		Growth Inhibition Assay		IC50=4.32581 μM	SANGER
CaR-1		Growth Inhibition Assay		IC50=68.25 nM	SANGER
CAS-1		Growth Inhibition Assay		IC50=207.44 nM	SANGER
Ca-Ski		Growth Inhibition Assay		IC50=156.39 nM	SANGER
CCRF-CEM		Growth Inhibition Assay		IC50=14.7809 μM	SANGER
CFPAC-1		Growth Inhibition Assay		IC50=150.66 nM	SANGER
CGTH-W-1		Growth Inhibition Assay		IC50=20.63 nM	SANGER
ChaGo-K-1		Growth Inhibition Assay		IC50=328.1 nM	SANGER
CHL-1		Growth Inhibition Assay		IC50=15.45 nM	SANGER
CHP-134		Growth Inhibition Assay		IC50=139.55 nM	SANGER
CHP-212		Growth Inhibition Assay		IC50=74.95 nM	SANGER
CO-314		Growth Inhibition Assay		IC50=38.74 nM	SANGER
COLO-320-HSR		Growth Inhibition Assay		IC50=403.37 nM	SANGER
COLO-668		Growth Inhibition Assay		IC50=706.1 nM	SANGER
COLO-678		Growth Inhibition Assay		IC50=2.83768 μM	SANGER
COLO-679		Growth Inhibition Assay		IC50=122.15 nM	SANGER
COLO-680N		Growth Inhibition Assay		IC50=110.76 nM	SANGER
COLO-684		Growth Inhibition Assay		IC50=33.58 nM	SANGER
COLO-741		Growth Inhibition Assay		IC50=1.49771 μM	SANGER
COLO-792		Growth Inhibition Assay		IC50=354.42 nM	SANGER
COLO-800		Growth Inhibition Assay		IC50=32.92 nM	SANGER
COLO-824		Growth Inhibition Assay		IC50=689.37 nM	SANGER
COLO-829		Growth Inhibition Assay		IC50=296.5 nM	SANGER
COR-L105		Growth Inhibition Assay		IC50=15.04 nM	SANGER
COR-L23		Growth Inhibition Assay		IC50=49.16 nM	SANGER
COR-L88		Growth Inhibition Assay		IC50=848.12 nM	SANGER
CP50-MEL-B		Growth Inhibition Assay		IC50=77.4 nM	SANGER
CTB-1		Growth Inhibition Assay		IC50=24.67 nM	SANGER
CTV-1		Growth Inhibition Assay		IC50=32.82 nM	SANGER
CW-2		Growth Inhibition Assay		IC50=269.96 nM	SANGER
D-247MG		Growth Inhibition Assay		IC50=135.21 nM	SANGER
D-263MG		Growth Inhibition Assay		IC50=29.35 nM	SANGER
D-283MED		Growth Inhibition Assay		IC50=49.61 nM	SANGER
D-392MG		Growth Inhibition Assay		IC50=107.54 nM	SANGER
D-423MG		Growth Inhibition Assay		IC50=52.08 nM	SANGER
D-502MG		Growth Inhibition Assay		IC50=105.7 nM	SANGER
D-56MG		Growth Inhibition Assay		IC50=17.69 nM	SANGER
Daoy		Growth Inhibition Assay		IC50=36.7 nM	SANGER
DB		Growth Inhibition Assay		IC50=27.36 nM	SANGER
DBTRG-05MG		Growth Inhibition Assay		IC50=198.47 nM	SANGER
DEL		Growth Inhibition Assay		IC50=20.49 nM	SANGER
Detroit562		Growth Inhibition Assay		IC50=102.17 nM	SANGER
DJM-1		Growth Inhibition Assay		IC50=340.33 nM	SANGER
DK-MG		Growth Inhibition Assay		IC50=180.3 nM	SANGER
DMS114	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.39 M	22336246
DMS-114		Growth Inhibition Assay		IC50=125.09 nM	SANGER
DMS273	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.80 M	22336246
DMS-273		Growth Inhibition Assay		IC50=60.87 nM	SANGER
DOHH-2		Growth Inhibition Assay		IC50=46.37 nM	SANGER
DOK		Growth Inhibition Assay		IC50=56.02 nM	SANGER
DoTc2-4510		Growth Inhibition Assay		IC50=1.07376 μM	SANGER
DSH1		Growth Inhibition Assay		IC50=406.91 nM	SANGER
DU145	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.16 M	22336246
DU-145		Growth Inhibition Assay		IC50=14.5052 μM	SANGER
DU-4475		Growth Inhibition Assay		IC50=9.44 nM	SANGER
ECC10		Growth Inhibition Assay		IC50=31.95 nM	SANGER
EFM-19		Growth Inhibition Assay		IC50=67.5 nM	SANGER
EFO-21		Growth Inhibition Assay		IC50=287.68 nM	SANGER
EFO-27		Growth Inhibition Assay		IC50=24.33 nM	SANGER
EGI-1		Growth Inhibition Assay		IC50=16.43 nM	SANGER
EKVX		Growth Inhibition Assay		IC50=100.6 nM	SANGER
EM-2		Growth Inhibition Assay		IC50=54.4 nM	SANGER
EoL-1		Growth Inhibition Assay		IC50=13.93 nM	SANGER
EPLC-272H		Growth Inhibition Assay		IC50=44.39 nM	SANGER
ES1		Growth Inhibition Assay		IC50=28.84 nM	SANGER
ES3		Growth Inhibition Assay		IC50=25.22 nM	SANGER
ES4		Growth Inhibition Assay		IC50=21.08 nM	SANGER
ES5		Growth Inhibition Assay		IC50=14.74 nM	SANGER
ES6		Growth Inhibition Assay		IC50=92.83 nM	SANGER
ES7		Growth Inhibition Assay		IC50=18.09 nM	SANGER
ES8		Growth Inhibition Assay		IC50=10.9 nM	SANGER
ESS-1		Growth Inhibition Assay		IC50=135.18 nM	SANGER
ETK-1		Growth Inhibition Assay		IC50=7.88 nM	SANGER
EW-1		Growth Inhibition Assay		IC50=120.2 nM	SANGER
EW-11		Growth Inhibition Assay		IC50=96.88 nM	SANGER
EW-13		Growth Inhibition Assay		IC50=95.75 nM	SANGER
EW-16		Growth Inhibition Assay		IC50=18.04 nM	SANGER
EW-18		Growth Inhibition Assay		IC50=31.86 nM	SANGER
EW-22		Growth Inhibition Assay		IC50=46.2 nM	SANGER
FADU		Growth Inhibition Assay		IC50=266.63 nM	SANGER
FTC-133		Growth Inhibition Assay		IC50=25.1 nM	SANGER
G-401		Growth Inhibition Assay		IC50=40.82 nM	SANGER
G-402		Growth Inhibition Assay		IC50=22.16 nM	SANGER
GAK		Growth Inhibition Assay		IC50=98.93 nM	SANGER
GAMG		Growth Inhibition Assay		IC50=19.48 nM	SANGER
GB-1		Growth Inhibition Assay		IC50=54.2 nM	SANGER
GCIY		Growth Inhibition Assay		IC50=50.67 nM	SANGER
GCT		Growth Inhibition Assay		IC50=13.68 nM	SANGER
GI-1		Growth Inhibition Assay		IC50=60.3 nM	SANGER
GI-ME-N		Growth Inhibition Assay		IC50=29.91 nM	SANGER
GMS-10		Growth Inhibition Assay		IC50=173.94 nM	SANGER
GOTO		Growth Inhibition Assay		IC50=250.29 nM	SANGER
GP5d		Growth Inhibition Assay		IC50=434.41 nM	SANGER
GR-ST		Growth Inhibition Assay		IC50=52.87 nM	SANGER
GT3TKB		Growth Inhibition Assay		IC50=118.08 nM	SANGER
H4		Growth Inhibition Assay		IC50=12.67 nM	SANGER
HAL-01		Growth Inhibition Assay		IC50=55.83 nM	SANGER
HBC4	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.61 M	22336246
HBC5	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.87 M	22336246
HCC1187		Growth Inhibition Assay		IC50=575.83 nM	SANGER
HCC1395		Growth Inhibition Assay		IC50=698.5 nM	SANGER
HCC1419		Growth Inhibition Assay		IC50=38.71 nM	SANGER
HCC1569		Growth Inhibition Assay		IC50=275.84 nM	SANGER
HCC1806		Growth Inhibition Assay		IC50=167.88 nM	SANGER
HCC1937		Growth Inhibition Assay		IC50=187.49 nM	SANGER
HCC1954		Growth Inhibition Assay		IC50=512.5 nM	SANGER
HCC2157		Growth Inhibition Assay		IC50=127.5 nM	SANGER
HCC2218		Growth Inhibition Assay		IC50=6.61 nM	SANGER
HCC2998	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.05 M	22336246
HCC2998		Growth Inhibition Assay		IC50=117.92 nM	SANGER
HCC38		Growth Inhibition Assay		IC50=266.48 nM	SANGER
HCC70		Growth Inhibition Assay		IC50=409.21 nM	SANGER
HCE-4		Growth Inhibition Assay		IC50=262.5 nM	SANGER
HCE-T		Growth Inhibition Assay		IC50=83.74 nM	SANGER
HCT116	0.01-100 μM	Growth Inhibition Assay	48 h	IC50=1.16 μM	23871904
HCT116	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.61 M	22336246
HCT-116		Growth Inhibition Assay		IC50=130.64 nM	SANGER
HCT15	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.03 M	22336246
HDLM-2		Growth Inhibition Assay		IC50=5.07725 μM	SANGER
HD-MY-Z		Growth Inhibition Assay		IC50=44.92 nM	SANGER
HEC-1		Growth Inhibition Assay		IC50=67.52 nM	SANGER
HEL		Growth Inhibition Assay		IC50=109.29 nM	SANGER
H-EMC-SS		Growth Inhibition Assay		IC50=146.81 nM	SANGER
HGC-27		Growth Inhibition Assay		IC50=18.06 nM	SANGER
HH		Growth Inhibition Assay		IC50=15.7 nM	SANGER
HL-60		Growth Inhibition Assay		IC50=123.1 nM	SANGER
HLE		Growth Inhibition Assay		IC50=53.47 nM	SANGER
HN		Growth Inhibition Assay		IC50=5.96 nM	SANGER
HO-1-N-1		Growth Inhibition Assay		IC50=25.15 nM	SANGER
HOP-92		Growth Inhibition Assay		IC50=26.48 nM	SANGER
HOS		Growth Inhibition Assay		IC50=21.06 nM	SANGER
HPAF-II		Growth Inhibition Assay		IC50=156.47 nM	SANGER
Hs-578-T		Growth Inhibition Assay		IC50=24.58 nM	SANGER
HSC-2		Growth Inhibition Assay		IC50=95.89 nM	SANGER
HSC-3		Growth Inhibition Assay		IC50=12.21 nM	SANGER
HT		Growth Inhibition Assay		IC50=41.02 nM	SANGER
HT-1080		Growth Inhibition Assay		IC50=21.93 nM	SANGER
HT-1197		Growth Inhibition Assay		IC50=238.09 nM	SANGER
HT-1376		Growth Inhibition Assay		IC50=384.88 nM	SANGER
HT-144		Growth Inhibition Assay		IC50=196.15 nM	SANGER
HT-29	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.75 M	22336246
HT-29		Growth Inhibition Assay		IC50=9.07599 μM	SANGER
HT55		Growth Inhibition Assay		IC50=1.31344 μM	SANGER
HTC-C3		Growth Inhibition Assay		IC50=116.85 nM	SANGER
HuCCT1		Growth Inhibition Assay		IC50=90.76 nM	SANGER
HuH-7		Growth Inhibition Assay		IC50=18.4 nM	SANGER
HuO-3N1		Growth Inhibition Assay		IC50=67.31 nM	SANGER
HuO9		Growth Inhibition Assay		IC50=26.76 nM	SANGER
HuP-T3		Growth Inhibition Assay		IC50=1.11905 μM	SANGER
HuP-T4		Growth Inhibition Assay		IC50=126.97 nM	SANGER
IA-LM		Growth Inhibition Assay		IC50=107.51 nM	SANGER
IGR-1		Growth Inhibition Assay		IC50=46.13 nM	SANGER
IGROV-1		Growth Inhibition Assay		IC50=135.76 nM	SANGER
IST-MEL1		Growth Inhibition Assay		IC50=18.77 nM	SANGER
IST-MES1		Growth Inhibition Assay		IC50=236.57 nM	SANGER
IST-SL1		Growth Inhibition Assay		IC50=1.4424 μM	SANGER
J82		Growth Inhibition Assay		IC50=185.18 nM	SANGER
JAR		Growth Inhibition Assay		IC50=956.24 nM	SANGER
JEG-3		Growth Inhibition Assay		IC50=84.1 nM	SANGER
J-RT3-T3-5		Growth Inhibition Assay		IC50=22.96 nM	SANGER
JVM-2		Growth Inhibition Assay		IC50=3.03188 μM	SANGER
JVM-3		Growth Inhibition Assay		IC50=30.83 nM	SANGER
K-562		Growth Inhibition Assay		IC50=28.4183 μM	SANGER
KALS-1		Growth Inhibition Assay		IC50=82.54 nM	SANGER
KARPAS-299		Growth Inhibition Assay		IC50=1.79479 μM	SANGER
KARPAS-45		Growth Inhibition Assay		IC50=13.51 nM	SANGER
KE-37		Growth Inhibition Assay		IC50=58.77 nM	SANGER
KG-1		Growth Inhibition Assay		IC50=84.24 nM	SANGER
KGN		Growth Inhibition Assay		IC50=56.32 nM	SANGER
KINGS-1		Growth Inhibition Assay		IC50=82.32 nM	SANGER
KLE		Growth Inhibition Assay		IC50=251.87 nM	SANGER
KM12	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.54 M	22336246
KM12		Growth Inhibition Assay		IC50=235.7 nM	SANGER
KM-H2		Growth Inhibition Assay		IC50=170.58 nM	SANGER
KNS-42		Growth Inhibition Assay		IC50=144.3 nM	SANGER
KNS-62		Growth Inhibition Assay		IC50=45.38 nM	SANGER
KNS-81-FD		Growth Inhibition Assay		IC50=19.54 nM	SANGER
KOSC-2		Growth Inhibition Assay		IC50=69.97 nM	SANGER
KP-4		Growth Inhibition Assay		IC50=7 nM	SANGER
KP-N-YN		Growth Inhibition Assay		IC50=14.5103 μM	SANGER
KP-N-YS		Growth Inhibition Assay		IC50=185 nM	SANGER
KS-1		Growth Inhibition Assay		IC50=44.66 nM	SANGER
KU-19-19		Growth Inhibition Assay		IC50=31.13 nM	SANGER
KU812		Growth Inhibition Assay		IC50=68.69 nM	SANGER
KURAMOCHI		Growth Inhibition Assay		IC50=265.9 nM	SANGER
KY821		Growth Inhibition Assay		IC50=56.2 nM	SANGER
KYSE-140		Growth Inhibition Assay		IC50=50.55 nM	SANGER
KYSE-150		Growth Inhibition Assay		IC50=25.89 nM	SANGER
KYSE-180		Growth Inhibition Assay		IC50=46.17 nM	SANGER
KYSE-270		Growth Inhibition Assay		IC50=130.88 nM	SANGER
KYSE-410		Growth Inhibition Assay		IC50=59.47 nM	SANGER
KYSE-450		Growth Inhibition Assay		IC50=55.16 nM	SANGER
KYSE-510		Growth Inhibition Assay		IC50=65.75 nM	SANGER
KYSE-520		Growth Inhibition Assay		IC50=252.86 nM	SANGER
KYSE-70		Growth Inhibition Assay		IC50=151.79 nM	SANGER
L-363		Growth Inhibition Assay		IC50=10.69 nM	SANGER
L-428		Growth Inhibition Assay		IC50=275.15 nM	SANGER
LAMA-84		Growth Inhibition Assay		IC50=35.87 nM	SANGER
LAN-6		Growth Inhibition Assay		IC50=6.21495 μM	SANGER
LB1047-RCC		Growth Inhibition Assay		IC50=38.81 nM	SANGER
LB2241-RCC		Growth Inhibition Assay		IC50=14.01 nM	SANGER
LB2518-MEL		Growth Inhibition Assay		IC50=157.1 nM	SANGER
LB771-HNC		Growth Inhibition Assay		IC50=285.84 nM	SANGER
LB831-BLC		Growth Inhibition Assay		IC50=120.63 nM	SANGER
LB996-RCC		Growth Inhibition Assay		IC50=47.19 nM	SANGER
LC-2-ad		Growth Inhibition Assay		IC50=158.62 nM	SANGER
LCLC-103H		Growth Inhibition Assay		IC50=285.99 nM	SANGER
LCLC-97TM1		Growth Inhibition Assay		IC50=82.86 nM	SANGER
LK-2		Growth Inhibition Assay		IC50=77.05 nM	SANGER
LN-405		Growth Inhibition Assay		IC50=63.85 nM	SANGER
LNCaP-Clone-FGC		Growth Inhibition Assay		IC50=37.59 nM	SANGER
LoVo		Growth Inhibition Assay		IC50=48.4 nM	SANGER
LOXIMVI	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.66 M	22336246
LOXIMVI		Growth Inhibition Assay		IC50=14.99 nM	SANGER
LS-1034		Growth Inhibition Assay		IC50=491.06 nM	SANGER
LS-123		Growth Inhibition Assay		IC50=92.18 nM	SANGER
LS-411N		Growth Inhibition Assay		IC50=187.28 nM	SANGER
LS-513		Growth Inhibition Assay		IC50=140.91 pM	SANGER
LU-134-A		Growth Inhibition Assay		IC50=79.03 nM	SANGER
LU-135		Growth Inhibition Assay		IC50=6.43077 μM	SANGER
LU-139		Growth Inhibition Assay		IC50=7.77 nM	SANGER
LU-65		Growth Inhibition Assay		IC50=1.62249 μM	SANGER
LU-99A		Growth Inhibition Assay		IC50=117.21 nM	SANGER
LXF-289		Growth Inhibition Assay		IC50=26.04 nM	SANGER
M059J		Growth Inhibition Assay		IC50=63.58 nM	SANGER
M14		Growth Inhibition Assay		IC50=60.04 nM	SANGER
MC116		Growth Inhibition Assay		IC50=57.8 nM	SANGER
MCF7	0.01-100 μM	Growth Inhibition Assay	48 h	IC50=0.73 μM	23871904
MCF7	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.16 M	22336246
MCF7		Growth Inhibition Assay		IC50=48.58 nM	SANGER
MC-IXC		Growth Inhibition Assay		IC50=70.08 nM	SANGER
MDA-MB-157		Growth Inhibition Assay		IC50=35.41 nM	SANGER
MDA-MB-175-VII		Growth Inhibition Assay		IC50=39.51 nM	SANGER
MDA-MB-231	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.09 M	22336246
MDA-MB-231		Growth Inhibition Assay		IC50=105.06 nM	SANGER
MDA-MB-361		Growth Inhibition Assay		IC50=61 nM	SANGER
MDA-MB-415		Growth Inhibition Assay		IC50=176.61 nM	SANGER
MDA-MB-453		Growth Inhibition Assay		IC50=3.10439 μM	SANGER
ME-180		Growth Inhibition Assay		IC50=22.43 nM	SANGER
MEG-01		Growth Inhibition Assay		IC50=63.52 nM	SANGER
MEL-HO		Growth Inhibition Assay		IC50=24.04 nM	SANGER
Mewo		Growth Inhibition Assay		IC50=11.99 nM	SANGER
MFE-280		Growth Inhibition Assay		IC50=9.99 nM	SANGER
MFM-223		Growth Inhibition Assay		IC50=131.51 nM	SANGER
MG-63		Growth Inhibition Assay		IC50=23.45 nM	SANGER
MHH-ESS-1		Growth Inhibition Assay		IC50=51.95 nM	SANGER
MHH-NB-11		Growth Inhibition Assay		IC50=629.01 nM	SANGER
MHH-PREB-1		Growth Inhibition Assay		IC50=9.12 nM	SANGER
MIA-PaCa-2		Growth Inhibition Assay		IC50=84.54 nM	SANGER
MKN1	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.41 M	22336246
MKN1		Growth Inhibition Assay		IC50=2.8 nM	SANGER
MKN28	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.07 M	22336246
MKN28		Growth Inhibition Assay		IC50=1.09024 μM	SANGER
MKN45	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.34 M	22336246
MKN7	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.68 M	22336246
MKN7		Growth Inhibition Assay		IC50=123.83 nM	SANGER
MKN74	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.42 M	22336246
ML-2		Growth Inhibition Assay		IC50=60.62 nM	SANGER
MLMA		Growth Inhibition Assay		IC50=136.58 nM	SANGER
MN-60		Growth Inhibition Assay		IC50=37.96 nM	SANGER
MOLT-13		Growth Inhibition Assay		IC50=113.44 nM	SANGER
MOLT-16		Growth Inhibition Assay		IC50=17.15 nM	SANGER
MOLT-4		Growth Inhibition Assay		IC50=25.12 nM	SANGER
Mo-T		Growth Inhibition Assay		IC50=947.88 nM	SANGER
MPP-89		Growth Inhibition Assay		IC50=25.32 nM	SANGER
MS-1		Growth Inhibition Assay		IC50=107.71 nM	SANGER
MSTO-211H		Growth Inhibition Assay		IC50=63.51 nM	SANGER
MV-4-11		Growth Inhibition Assay		IC50=28.7 nM	SANGER
MZ1-PC		Growth Inhibition Assay		IC50=205.58 nM	SANGER
MZ2-MEL		Growth Inhibition Assay		IC50=39.66 nM	SANGER
MZ7-mel		Growth Inhibition Assay		IC50=323.76 nM	SANGER
NB10		Growth Inhibition Assay		IC50=240.06 nM	SANGER
NB12		Growth Inhibition Assay		IC50=528.42 nM	SANGER
NB13		Growth Inhibition Assay		IC50=117.99 nM	SANGER
NB14		Growth Inhibition Assay		IC50=88.3 nM	SANGER
NB17		Growth Inhibition Assay		IC50=721.75 nM	SANGER
NB5		Growth Inhibition Assay		IC50=40.64 nM	SANGER
NB6		Growth Inhibition Assay		IC50=396.66 nM	SANGER
NB69		Growth Inhibition Assay		IC50=22.53 nM	SANGER
NB7		Growth Inhibition Assay		IC50=189.89 nM	SANGER
NBsusSR		Growth Inhibition Assay		IC50=24.6 nM	SANGER
NCI-H1048		Growth Inhibition Assay		IC50=86.31 nM	SANGER
NCI-H1092		Growth Inhibition Assay		IC50=144.52 nM	SANGER
NCI-H1155		Growth Inhibition Assay		IC50=48.32 nM	SANGER
NCI-H1299		Growth Inhibition Assay		IC50=150.22 nM	SANGER
NCI-H1304		Growth Inhibition Assay		IC50=1.65498 μM	SANGER
NCI-H1355		Growth Inhibition Assay		IC50=46.34 nM	SANGER
NCI-H1395		Growth Inhibition Assay		IC50=198.85 nM	SANGER
NCI-H1437		Growth Inhibition Assay		IC50=80.5 nM	SANGER
NCI-H1563		Growth Inhibition Assay		IC50=105.18 nM	SANGER
NCI-H1573		Growth Inhibition Assay		IC50=87.48 nM	SANGER
NCI-H1581		Growth Inhibition Assay		IC50=64.03 nM	SANGER
NCI-H1623		Growth Inhibition Assay		IC50=47.76 nM	SANGER
NCI-H1648		Growth Inhibition Assay		IC50=113 nM	SANGER
NCI-H1650		Growth Inhibition Assay		IC50=204.01 nM	SANGER
NCI-H1651		Growth Inhibition Assay		IC50=344.18 nM	SANGER
NCI-H1666		Growth Inhibition Assay		IC50=9.71 nM	SANGER
NCI-H1693		Growth Inhibition Assay		IC50=136.12 nM	SANGER
NCI-H1755		Growth Inhibition Assay		IC50=138.85 nM	SANGER
NCI-H1770		Growth Inhibition Assay		IC50=326.74 nM	SANGER
NCI-H1792		Growth Inhibition Assay		IC50=66.15 nM	SANGER
NCI-H1793		Growth Inhibition Assay		IC50=12.82 nM	SANGER
NCI-H1838		Growth Inhibition Assay		IC50=1.02388 μM	SANGER
NCI-H1993		Growth Inhibition Assay		IC50=10.5081 μM	SANGER
NCI-H2029		Growth Inhibition Assay		IC50=1.41791 μM	SANGER
NCI-H2030		Growth Inhibition Assay		IC50=21.52 nM	SANGER
NCI-H2052		Growth Inhibition Assay		IC50=174.9 nM	SANGER
NCI-H2087		Growth Inhibition Assay		IC50=234.51 nM	SANGER
NCI-H209		Growth Inhibition Assay		IC50=17.29 nM	SANGER
NCI-H2122		Growth Inhibition Assay		IC50=200.59 nM	SANGER
NCI-H2126		Growth Inhibition Assay		IC50=148.15 nM	SANGER
NCI-H2170		Growth Inhibition Assay		IC50=114.51 nM	SANGER
NCI-H2228		Growth Inhibition Assay		IC50=88.26 nM	SANGER
NCI-H226	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.44 M	22336246
NCI-H226		Growth Inhibition Assay		IC50=707.8 nM	SANGER
NCI-H2291		Growth Inhibition Assay		IC50=598.31 nM	SANGER
NCI-H23	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.64 M	22336246
NCI-H23		Growth Inhibition Assay		IC50=219.33 nM	SANGER
NCI-H2342		Growth Inhibition Assay		IC50=590.39 nM	SANGER
NCI-H2347		Growth Inhibition Assay		IC50=172.72 nM	SANGER
NCI-H2405		Growth Inhibition Assay		IC50=54.88 nM	SANGER
NCI-H2452		Growth Inhibition Assay		IC50=44.58 nM	SANGER
NCI-H28		Growth Inhibition Assay		IC50=34.44 nM	SANGER
NCI-H292		Growth Inhibition Assay		IC50=27 nM	SANGER
NCI-H358		Growth Inhibition Assay		IC50=1.95503 μM	SANGER
NCI-H438	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.11 M	22336246
NCI-H441		Growth Inhibition Assay		IC50=895.22 nM	SANGER
NCI-H446		Growth Inhibition Assay		IC50=95.12 nM	SANGER
NCI-H460		Growth Inhibition Assay		IC50=81.23 nM	SANGER
NCI-H520		Growth Inhibition Assay		IC50=83.06 nM	SANGER
NCI-H522	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.45 M	22336246
NCI-H522		Growth Inhibition Assay		IC50=248.31 nM	SANGER
NCI-H526		Growth Inhibition Assay		IC50=823.53 nM	SANGER
NCI-H596		Growth Inhibition Assay		IC50=228.22 nM	SANGER
NCI-H630		Growth Inhibition Assay		IC50=912.96 nM	SANGER
NCI-H650		Growth Inhibition Assay		IC50=94.09 nM	SANGER
NCI-H661		Growth Inhibition Assay		IC50=151.26 nM	SANGER
NCI-H69		Growth Inhibition Assay		IC50=426.76 nM	SANGER
NCI-H720		Growth Inhibition Assay		IC50=3.57 nM	SANGER
NCI-H727		Growth Inhibition Assay		IC50=412.11 nM	SANGER
NCI-H747		Growth Inhibition Assay		IC50=119.34 nM	SANGER
NCI-H810		Growth Inhibition Assay		IC50=278.31 nM	SANGER
NCI-H82		Growth Inhibition Assay		IC50=2.90369 μM	SANGER
NCI-N87		Growth Inhibition Assay		IC50=111.04 nM	SANGER
NCI-SNU-1		Growth Inhibition Assay		IC50=21.95 nM	SANGER
NCI-SNU-5		Growth Inhibition Assay		IC50=336.77 nM	SANGER
NEC8		Growth Inhibition Assay		IC50=67.24 nM	SANGER
NH-12		Growth Inhibition Assay		IC50=132.99 nM	SANGER
NKM-1		Growth Inhibition Assay		IC50=54.81 nM	SANGER
NMC-G1		Growth Inhibition Assay		IC50=121.11 nM	SANGER
no-10		Growth Inhibition Assay		IC50=201.04 nM	SANGER
no-11		Growth Inhibition Assay		IC50=113.28 nM	SANGER
NOMO-1		Growth Inhibition Assay		IC50=45.87 nM	SANGER
NOS-1		Growth Inhibition Assay		IC50=30.12 nM	SANGER
NTERA-S-cl-D1		Growth Inhibition Assay		IC50=43 nM	SANGER
NUGC-3		Growth Inhibition Assay		IC50=16.34 nM	SANGER
NY		Growth Inhibition Assay		IC50=1.16792 μM	SANGER
OAW-28		Growth Inhibition Assay		IC50=2.06919 μM	SANGER
OAW-42		Growth Inhibition Assay		IC50=73.39 nM	SANGER
OCI-AML2		Growth Inhibition Assay		IC50=82.61 nM	SANGER
OCUB-M		Growth Inhibition Assay		IC50=82.41 nM	SANGER
OE19		Growth Inhibition Assay		IC50=340.53 nM	SANGER
OE33		Growth Inhibition Assay		IC50=188.97 nM	SANGER
OMC-1		Growth Inhibition Assay		IC50=100.18 nM	SANGER
ONS-76		Growth Inhibition Assay		IC50=29.05 nM	SANGER
OS-RC-2		Growth Inhibition Assay		IC50=16.47 nM	SANGER
OVCAR3	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.17 M	22336246
OVCAR-3		Growth Inhibition Assay		IC50=598.96 nM	SANGER
OVCAR4	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.58 M	22336246
OVCAR-4		Growth Inhibition Assay		IC50=73.36 nM	SANGER
OVCAR5	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.57 M	22336246
OVCAR-5		Growth Inhibition Assay		IC50=35.47 nM	SANGER
OVCAR8	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.84 M	22336246
OVCAR-8		Growth Inhibition Assay		IC50=31.26 nM	SANGER
P12-ICHIKAWA		Growth Inhibition Assay		IC50=15.1 nM	SANGER
P30-OHK		Growth Inhibition Assay		IC50=83.5 nM	SANGER
PA-1		Growth Inhibition Assay		IC50=11.82 nM	SANGER
PANC-03-27		Growth Inhibition Assay		IC50=76.25 nM	SANGER
PANC-08-13		Growth Inhibition Assay		IC50=58.01 nM	SANGER
PANC-10-05		Growth Inhibition Assay		IC50=245.56 nM	SANGER
PC-14		Growth Inhibition Assay		IC50=46.57 nM	SANGER
PC3	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.66 M	22336246
PC-3		Growth Inhibition Assay		IC50=5.09 nM	SANGER
PFSK-1		Growth Inhibition Assay		IC50=49.06 nM	SANGER
PSN1		Growth Inhibition Assay		IC50=44.4 nM	SANGER
QIMR-WIL		Growth Inhibition Assay		IC50=30.6 nM	SANGER
Ramos-2G6-4C10		Growth Inhibition Assay		IC50=8.49 nM	SANGER
RCC10RGB		Growth Inhibition Assay		IC50=224.19 nM	SANGER
RCM-1		Growth Inhibition Assay		IC50=496.68 nM	SANGER
RD		Growth Inhibition Assay		IC50=75.86 nM	SANGER
RERF-LC-MS		Growth Inhibition Assay		IC50=124.31 nM	SANGER
RH-1		Growth Inhibition Assay		IC50=54.7 nM	SANGER
RH-18		Growth Inhibition Assay		IC50=394.74 nM	SANGER
RKO		Growth Inhibition Assay		IC50=38.33 nM	SANGER
RMG-I		Growth Inhibition Assay		IC50=467.56 nM	SANGER
RO82-W-1		Growth Inhibition Assay		IC50=59.9 nM	SANGER
RPMI-2650		Growth Inhibition Assay		IC50=52.69 nM	SANGER
RPMI-7951		Growth Inhibition Assay		IC50=19.28 nM	SANGER
RPMI-8226		Growth Inhibition Assay		IC50=33.82 nM	SANGER
RPMI-8866		Growth Inhibition Assay		IC50=72.82 nM	SANGER
RS4-11		Growth Inhibition Assay		IC50=26.91 nM	SANGER
RT-112		Growth Inhibition Assay		IC50=19.66 nM	SANGER
RVH-421		Growth Inhibition Assay		IC50=53.67 nM	SANGER
RXF393		Growth Inhibition Assay		IC50=21.45 nM	SANGER
RXF631L	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.21 M	22336246
S-117		Growth Inhibition Assay		IC50=76.27 nM	SANGER
Saos-2		Growth Inhibition Assay		IC50=179.35 nM	SANGER
SAS		Growth Inhibition Assay		IC50=652.67 nM	SANGER
SBC-1		Growth Inhibition Assay		IC50=742 pM	SANGER
SBC-5		Growth Inhibition Assay		IC50=83.52 nM	SANGER
SCC-15		Growth Inhibition Assay		IC50=173.66 nM	SANGER
SCC-25		Growth Inhibition Assay		IC50=89.82 nM	SANGER
SCC-4		Growth Inhibition Assay		IC50=71.38 nM	SANGER
SCC-9		Growth Inhibition Assay		IC50=293.22 nM	SANGER
SCH		Growth Inhibition Assay		IC50=67.1 nM	SANGER
SF126		Growth Inhibition Assay		IC50=19.41 nM	SANGER
SF268	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.92 M	22336246
SF268		Growth Inhibition Assay		IC50=102.34 nM	SANGER
SF295	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.31 M	22336246
SF295		Growth Inhibition Assay		IC50=18.93 nM	SANGER
SF539	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.59 M	22336246
SF539		Growth Inhibition Assay		IC50=52.35 nM	SANGER
SH-4		Growth Inhibition Assay		IC50=75.21 nM	SANGER
SHP-77		Growth Inhibition Assay		IC50=3.528 μM	SANGER
SiHa		Growth Inhibition Assay		IC50=329.24 nM	SANGER
SJRH30		Growth Inhibition Assay		IC50=144.44 nM	SANGER
SJSA-1		Growth Inhibition Assay		IC50=38.54 nM	SANGER
SKG-IIIa		Growth Inhibition Assay		IC50=128.8 nM	SANGER
SK-HEP-1		Growth Inhibition Assay		IC50=46.04 nM	SANGER
SK-LU-1		Growth Inhibition Assay		IC50=26.17 nM	SANGER
SK-MEL-1		Growth Inhibition Assay		IC50=11.6289 μM	SANGER
SK-MEL-2		Growth Inhibition Assay		IC50=76.75 nM	SANGER
SK-MEL-24		Growth Inhibition Assay		IC50=516.51 nM	SANGER
SK-MEL-28		Growth Inhibition Assay		IC50=111.55 nM	SANGER
SK-MEL-3		Growth Inhibition Assay		IC50=147.55 nM	SANGER
SK-MEL-30		Growth Inhibition Assay		IC50=196.2 nM	SANGER
SK-MES-1		Growth Inhibition Assay		IC50=53.26 nM	SANGER
SK-N-AS		Growth Inhibition Assay		IC50=137.17 nM	SANGER
SK-N-DZ		Growth Inhibition Assay		IC50=2.86381 μM	SANGER
SK-NEP-1		Growth Inhibition Assay		IC50=34.15 nM	SANGER
SK-N-FI		Growth Inhibition Assay		IC50=147.59 nM	SANGER
SKOV3	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.41 M	22336246
SK-OV-3		Growth Inhibition Assay		IC50=100.07 nM	SANGER
SK-PN-DW		Growth Inhibition Assay		IC50=235.19 nM	SANGER
SN12C		Growth Inhibition Assay		IC50=90.62 nM	SANGER
SNB75	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.58 M	22336246
SNB75		Growth Inhibition Assay		IC50=54.26 nM	SANGER
SNB78	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-8.65 M	22336246
SNU-387		Growth Inhibition Assay		IC50=104.17 nM	SANGER
SNU-423		Growth Inhibition Assay		IC50=67.98 nM	SANGER
SNU-449		Growth Inhibition Assay		IC50=75.79 nM	SANGER
SNU-C2B		Growth Inhibition Assay		IC50=180.73 nM	SANGER
St-4	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.47 M	22336246
SW1088		Growth Inhibition Assay		IC50=28.29 nM	SANGER
SW1116		Growth Inhibition Assay		IC50=3.05411 μM	SANGER
SW13		Growth Inhibition Assay		IC50=66.5 nM	SANGER
SW1417		Growth Inhibition Assay		IC50=7.91731 μM	SANGER
SW1463		Growth Inhibition Assay		IC50=739.19 nM	SANGER
SW1573		Growth Inhibition Assay		IC50=109.31 nM	SANGER
SW1710		Growth Inhibition Assay		IC50=18.72 nM	SANGER
SW1783		Growth Inhibition Assay		IC50=110.22 nM	SANGER
SW1990		Growth Inhibition Assay		IC50=108.54 nM	SANGER
SW48		Growth Inhibition Assay		IC50=201.31 nM	SANGER
SW620		Growth Inhibition Assay		IC50=50.36 nM	SANGER
SW626		Growth Inhibition Assay		IC50=176.06 nM	SANGER
SW684		Growth Inhibition Assay		IC50=196.13 nM	SANGER
SW756		Growth Inhibition Assay		IC50=554.96 nM	SANGER
SW780		Growth Inhibition Assay		IC50=23.13 nM	SANGER
SW837		Growth Inhibition Assay		IC50=1.32978 μM	SANGER
SW872		Growth Inhibition Assay		IC50=64.57 nM	SANGER
SW900		Growth Inhibition Assay		IC50=154.65 nM	SANGER
SW948		Growth Inhibition Assay		IC50=4.74779 μM	SANGER
SW954		Growth Inhibition Assay		IC50=233.83 nM	SANGER
SW962		Growth Inhibition Assay		IC50=26.76 nM	SANGER
SW982		Growth Inhibition Assay		IC50=49.91 nM	SANGER
T-24		Growth Inhibition Assay		IC50=43.83 nM	SANGER
T47D		Growth Inhibition Assay		IC50=67.87 nM	SANGER
T84		Growth Inhibition Assay		IC50=6.9864 μM	SANGER
T98G		Growth Inhibition Assay		IC50=29.88 nM	SANGER
TCCSUP		Growth Inhibition Assay		IC50=64.53 nM	SANGER
TE-1		Growth Inhibition Assay		IC50=222.88 nM	SANGER
TE-10		Growth Inhibition Assay		IC50=407.01 nM	SANGER
TE-11		Growth Inhibition Assay		IC50=55.99 nM	SANGER
TE-12		Growth Inhibition Assay		IC50=140.93 nM	SANGER
TE-5		Growth Inhibition Assay		IC50=46.84 nM	SANGER
TE-6		Growth Inhibition Assay		IC50=219.68 nM	SANGER
TE-8		Growth Inhibition Assay		IC50=66.52 nM	SANGER
TE-9		Growth Inhibition Assay		IC50=1.12973 μM	SANGER
TGBC11TKB		Growth Inhibition Assay		IC50=410.33 nM	SANGER
TGBC1TKB		Growth Inhibition Assay		IC50=23.05 nM	SANGER
TGBC24TKB		Growth Inhibition Assay		IC50=222.17 nM	SANGER
TGW		Growth Inhibition Assay		IC50=760.15 nM	SANGER
TH-3		Growth Inhibition Assay		IC50=379.95 nM	SANGER
TI-73		Growth Inhibition Assay		IC50=25.28 nM	SANGER
TK10		Growth Inhibition Assay		IC50=100.21 nM	SANGER
Trypanosoma brucei brucei		Antimicrobial Assay	18 h	Antitrypanosomal activity with EC50 of 0.0025 μM	24805946
Trypanosoma brucei brucei	200 nM	Function Assay	12 h	Decrease in phosphotidyl inositol phosphate level	24805946
Trypanosoma brucei brucei		Function Assay	18 h	Inhibition of receptor-mediated endocytosis assessed as decrease in transferrin uptake	24805946
Trypanosoma brucei brucei	200 nM	Function Assay	12 h	Effect on sphingomylein level	24805946
Trypanosoma brucei brucei	200 nM	Function Assay	12 h	Effect on phosphatidylcholine level	24805946
TYK-nu		Growth Inhibition Assay		IC50=9.94 nM	SANGER
U031		Growth Inhibition Assay		IC50=96.73 nM	SANGER
U-118-MG		Growth Inhibition Assay		IC50=133.62 nM	SANGER
U251	0.01-100 μM	Growth Inhibition Assay	48 h	Log GI50=-7.66 M	22336246
U251		Growth Inhibition Assay		IC50=38.43 nM	SANGER
U-266		Growth Inhibition Assay		IC50=205.79 nM	SANGER
U-2-OS		Growth Inhibition Assay		IC50=29.5 nM	SANGER
U87MG	0.01-100 μM	Growth Inhibition Assay	48 h	IC50=1.32 μM	23871904
U-87-MG		Growth Inhibition Assay		IC50=300.73 nM	SANGER
UACC-257		Growth Inhibition Assay		IC50=213.99 nM	SANGER
UACC-62		Growth Inhibition Assay		IC50=168.09 nM	SANGER
UACC-893		Growth Inhibition Assay		IC50=406.47 nM	SANGER
UMC-11		Growth Inhibition Assay		IC50=458.36 nM	SANGER
UM-UC-3		Growth Inhibition Assay		IC50=315 pM	SANGER
VA-ES-BJ		Growth Inhibition Assay		IC50=17.83 nM	SANGER
VM-CUB-1		Growth Inhibition Assay		IC50=33.43 nM	SANGER
VMRC-RCZ		Growth Inhibition Assay		IC50=15.63 nM	SANGER
WM-115		Growth Inhibition Assay		IC50=68.14 nM	SANGER
YAPC		Growth Inhibition Assay		IC50=490.6 nM	SANGER
YH-13		Growth Inhibition Assay		IC50=21.88 nM	SANGER
YKG-1		Growth Inhibition Assay		IC50=53 nM	SANGER
ZR-75-30		Growth Inhibition Assay		IC50=16.3303 μM	SANGER
22RV1		Growth Inhibition Assay		IC50=49.09 nM	SANGER
5637		Growth Inhibition Assay		IC50=79.23 nM	SANGER
639-V		Growth Inhibition Assay		IC50=85.42 nM	SANGER
647-V		Growth Inhibition Assay		IC50=78.07 nM	SANGER
697		Growth Inhibition Assay		IC50=17.43 nM	SANGER
769-P		Growth Inhibition Assay		IC50=10.44 nM	SANGER
786-0		Growth Inhibition Assay		IC50=22.29 nM	SANGER
8305C		Growth Inhibition Assay		IC50=41.87 nM	SANGER
8505C		Growth Inhibition Assay		IC50=37.51 nM	SANGER
8-MG-BA		Growth Inhibition Assay		IC50=37.25 nM	SANGER
A101D		Growth Inhibition Assay		IC50=38.97 nM	SANGER
A204		Growth Inhibition Assay		IC50=28.47 nM	SANGER
A2058		Growth Inhibition Assay		IC50=33.25 nM	SANGER
A253		Growth Inhibition Assay		IC50=82.65 nM	SANGER
A2780		Growth Inhibition Assay		IC50=106.47 nM	SANGER
A375		Growth Inhibition Assay		IC50=23.93 nM	SANGER
A388		Growth Inhibition Assay		IC50=249.82 nM	SANGER

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01285466	Metastatic or Locally Advanced... 展开 >> Solid Tumors 收起 <<	Phase 1	Completed	-	Belgium ... 展开 >> Novartis Investigative Site Bruxelles, Belgium, 1000 Novartis Investigative Site Bruxelles, Belgium, 1200 Novartis Investigative Site Wilrijk, Belgium, 2610 Germany Novartis Investigative Site Essen, Germany, 45147 Novartis Investigative Site Köln, Germany, 50937 Netherlands Novartis Investigative Site Amsterdam, Netherlands, 1066 CX Spain Novartis Investigative Site Sevilla, Andalucia, Spain, 41013 Novartis Investigative Site Barcelona, Catalunya, Spain, 08035 Switzerland Novartis Investigative Site Chur, Switzerland, 7000 Novartis Investigative Site St. Gallen, Switzerland, 9007 收起 <<
NCT02430363	Glioblastoma	Phase 1 Phase 2	Unknown	June 2018	United States, Massachusetts ... 展开 >> Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Texas M D Anderson Cancer Center Houston, Texas, United States, 77030 Belgium UCL- Cliniques Universitaires Saint Luc Brussels, Belgium Germany St Johannes Hospital Duisburg, Germany, 47166 Italy Spedali Civili di Brescia Brescia, Italy IRCCS San Raffaele Milan, Italy Poland Lower-Silesian Oncology Centre Wroclaw, Lower-Silesian, Poland, 53413 Russian Federation Pavlov State Medical University St. Petersburg, Russian Federation, 197089 Spain Hospital Universitario Germans Trias I Pujol Barcelona,, Spain Switzerland Universitätsklinik für Frauenheilkunde Bern, Switzerland Ukraine Regional Cancer Center Dnepropetrovsk, Ukraine, 49000 National Institute of Cancer Kiev, Ukraine, 03035 United Kingdom Royal Victoria Hospital Belfast, Ulster, United Kingdom, BT12 6BA 收起 <<
NCT01508104	Cancer	Phase 1	Terminated(funding)	-	United States, Ohio ... 展开 >> University of Cincinnati Cincinnati, Ohio, United States, 45267-0502 收起 <<
NCT00620594	Breast Cancer ... 展开 >> Advanced Solid Tumors Cowden Syndrome 收起 <<	Phase 1	Completed	-	United States, California ... 展开 >> University of California at Los Angeles JonssonComprehensiveCancerCtr Los Angeles, California, United States, 90095 United States, Connecticut Yale University School of Medicine YaleCancerCtr-ClinTrialsOffice New Haven, Connecticut, United States, 06520 United States, Massachusetts Dana Farber Cancer Institute Clinical Trials ProjectManager Boston, Massachusetts, United States, 02215 United States, Nevada Nevada Cancer Institute NVCC - Huntsman Las Vegas, Nevada, United States, 89135 United States, South Carolina Cancer Centers of the Carolinas CCC Faris Greenville, South Carolina, United States, 29605 United States, Tennessee Sarah Cannon Research Institute Dept.ofSarahCannonCancerCtr(2) Nashville, Tennessee, United States, 37203 United States, Texas Baylor Health Care System/Sammons Cancer Center Baylor- Sammons Dallas, Texas, United States, 75246 University of Texas/MD Anderson Cancer Center Thoractic Head/Neck Med.Onc(2) Houston, Texas, United States, 77030-4009 Tyler Cancer Center TCC Tyler, Texas, United States, 75702 Germany Novartis Investigative Site Essen, Germany, 45147 Netherlands Novartis Investigative Site Amsterdam, Netherlands, 1066 CX Spain Novartis Investigative Site Barcelona, Catalunya, Spain, 08035 Novartis Investigative Site Valencia, Comunidad Valenciana, Spain, 46009 Novartis Investigative Site Valencia, Comunidad Valenciana, Spain, 46010 United Kingdom Novartis Investigative Site Manchester, United Kingdom, M20 9BX 收起 <<
NCT01471847	Locally Advance Breast Cancer ... 展开 >>(LABC) Metastatic Breast Cancer (MBC) 收起 <<	Phase 1	Completed	-	Spain ... 展开 >> Novartis Investigative Site Madrid, Spain, 28050 United Kingdom Novartis Investigative Site Leicester, United Kingdom, LE1 5WW Novartis Investigative Site Manchester, United Kingdom, M20 2BX 收起 <<
NCT01300962	Metastatic Breast Cancer	Phase 1	Active, not recruiting	December 2018	United States, North Carolina ... 展开 >> Lineberger Comprehensive Cancer Center Chapel Hill, North Carolina, United States, 27599 Duke Comprehensive Cancer Center Durham, North Carolina, United States, 27710 收起 <<
NCT01337765	Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific Solid Tumor 收起 <<	Phase 1	Completed	-	United States, Massachusetts ... 展开 >> Massachusetts General Hospital Mass General 2 Boston, Massachusetts, United States, 02114 United States, Texas University of Texas/MD Anderson Cancer Center MD Anderson PSC Houston, Texas, United States, 77030-4009 Australia, Victoria Novartis Investigative Site Parkville, Victoria, Australia, 3050 Canada, Ontario Novartis Investigative Site Toronto, Ontario, Canada, M5G 2M9 France Novartis Investigative Site Villejuif Cedex, France, 94805 Spain Novartis Investigative Site Barcelona, Cataluña, Spain, 08035 收起 <<
NCT01288092	Metastatic Breast Cancer	Phase 2	Withdrawn	-	-
NCT01195376	Advanced Solid Tumor	Phase 1	Completed	-	Japan ... 展开 >> Novartis Investigative Site Kobe-city, Hyogo, Japan, 650-0017 Novartis Investigative Site Yufu, Oita, Japan, 879-5593 收起 <<
NCT01634061	Castration-resistant Prostate ... 展开 >>Cancer 收起 <<	Phase 1	Completed	-	United States, California ... 展开 >> Cedars Sinai Medical Center SC Los Angeles, California, United States, 90048 United States, New Jersey Hackensack University Medical Center Hackensack Univ Hackensack, New Jersey, United States, 07601 Belgium Novartis Investigative Site Brussels, Belgium, BE-B-1200 Novartis Investigative Site Wilrijk, Belgium, 2610 Canada, British Columbia Novartis Investigative Site Vancouver, British Columbia, Canada, V5Z 4E6 France Novartis Investigative Site Marseille, France, 13273 Novartis Investigative Site Villejuif Cedex, France, 94805 Spain Novartis Investigative Site Barcelona, Catalunya, Spain, 08036 Novartis Investigative Site Madrid, Spain, 28041 United Kingdom Novartis Investigative Site Sutton, United Kingdom, SM2 5PT 收起 <<
NCT03373903	Respiratory Tract Infections	Phase 2	Active, not recruiting	July 2018	United States, Kansas ... 展开 >> Heartland Research Associates Wichita, Kansas, United States, 67205 收起 <<
NCT01495247	Inoperable Locally Advanced Br... 展开 >>east Cancer Metastatic Breast Cancer (MBC) 收起 <<	Phase 1 Phase 2	Completed	-	France ... 展开 >> Novartis Investigative Site Dijon Cedex, France, 21034 Novartis Investigative Site Saint-Herblain Cédex, France, 44805 Spain Novartis Investigative Site Hospitalet de LLobregat, Catalunya, Spain, 08907 收起 <<
NCT01628913	Pancreatic Neuroendocrine Tumo... 展开 >>rs (pNET) 收起 <<	Phase 2	Terminated(This trial was term... 展开 >>inated based on an interim analysis as BEZ235 did not demonstrate a progression free survival advantage to everolimus treatment.) 收起 <<	-	United States, California ... 展开 >> Cedars Sinai Medical Center SC-3 Los Angeles, California, United States, 90048 United States, Colorado University of Colorado Univ Colorado Aurora, Colorado, United States, 80045 United States, Kentucky University of Kentucky Univ Kebtucky Lexington, Kentucky, United States, 40536-0098 United States, New York Montefiore Medical Center SC Bronx, New York, United States, 10467 France Novartis Investigative Site Lyon, France, 69437 Novartis Investigative Site Montpellier Cedex 5, France, 34298 Novartis Investigative Site Paris, France, 75015 Novartis Investigative Site Reims, France, 51092 Novartis Investigative Site Toulouse Cedex 4, France, 31054 Italy Novartis Investigative Site Bologna, BO, Italy, 40138 Novartis Investigative Site Pisa, PI, Italy, 56126 Novartis Investigative Site Roma, RM, Italy, 00189 Netherlands Novartis Investigative Site Amsterdam, Netherlands, 1105 AZ Novartis Investigative Site Groningen, Netherlands, 9713 GZ Russian Federation Novartis Investigative Site Kazan, Russian Federation, 420029 Spain Novartis Investigative Site Sevilla, Andalucia, Spain, 41013 Novartis Investigative Site Barcelona, Catalunya, Spain, 08035 Novartis Investigative Site Hospitalet de LLobregat, Catalunya, Spain, 08907 Novartis Investigative Site Madrid, Spain, 28034 Novartis Investigative Site Madrid, Spain, 28046 Switzerland Novartis Investigative Site Luzern, Switzerland, 6000 United Kingdom Novartis Investigative Site Glasgow, United Kingdom, G11 6NT Novartis Investigative Site London, United Kingdom, NW3 2QG Novartis Investigative Site London, United Kingdom, SE1 9RT Novartis Investigative Site Manchester, United Kingdom, M20 9BX Novartis Investigative Site Sheffield, United Kingdom, S10 2SJ 收起 <<
NCT01290406	Endometrial Cancer	Phase 2	Withdrawn	December 2017	-
NCT01482156	Advanced Solid Tumors ... 展开 >> Metastatic Breast Cancer Metastatic Renal Cell Carcinoma 收起 <<	Phase 1	Completed	-	United States, Arkansas ... 展开 >> Highlands Oncology Group Dept of Highlands Oncology Grp Fayetteville, Arkansas, United States, 72703 United States, Missouri Washington University School of Medicine Washington University (16) St. Louis, Missouri, United States, 63110 United States, South Carolina Medical University of South Carolina SC Charleston, South Carolina, United States, 29425 Belgium Novartis Investigative Site Wilrijk, Belgium, 2610 France Novartis Investigative Site Bordeaux Cedex, France, 33075 Novartis Investigative Site Montellier cedex 5, France, 34298 Italy Novartis Investigative Site Verona, VR, Italy, 37126 New Zealand Novartis Investigative Site Auckland, New Zealand Spain Novartis Investigative Site Barcelona, Catalunya, Spain, 08035 United Kingdom Novartis Investigative Site High Heaton, Newcastle Upon Tyne, United Kingdom, NE7 7DN 收起 <<
NCT01756118	Acute Lymphoblastic Leukemia ... 展开 >> Leukemia, Myelocytic, Acute Chronic Myelogenous Leukemia With Crisis of Blast Cells 收起 <<	Phase 1	Active, not recruiting	December 2017	Germany ... 展开 >> Johann Wolfgang Goethe University Hospitals Frankfurt, Hessen, Germany, 60590 收起 <<
NCT01690871	Malignant PEComa (Perivascular... 展开 >> Epithelioid Cell Tumors) 收起 <<	Phase 2	Withdrawn	January 2015	Spain ... 展开 >> Novartis Investigative Site Barcelona, Cataluña, Spain, 08025 收起 <<
NCT01453595	Renal Cancer	Phase 1 Phase 2	Terminated(Given the number of... 展开 >> toxicities seen and the difficulty with patient retention in the dose escalation portion, the sponsor decided to close the trial.) 收起 <<	-	United States, New York ... 展开 >> Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 收起 <<
NCT01628913	-		Terminated(This trial was term... 展开 >>inated based on an interim analysis as BEZ235 did not demonstrate a progression free survival advantage to everolimus treatment.) 收起 <<	-	-
NCT01658436	Pancreatic Neuroendocrine Tumo... 展开 >>rs (pNET) 收起 <<	Phase 2	Completed	-	United States, Indiana ... 展开 >> Indiana University SC Indianapolis, Indiana, United States, 46202 United States, Massachusetts Dana Farber Cancer Institute GastrointestionalCancer Clinic Boston, Massachusetts, United States, 02215 United States, New York Montefiore Medical Center SC-2 Bronx, New York, United States, 10467 United States, Ohio Ohio State Comprehensive Cancer Center/James Cancer Hospital SC Columbus, Ohio, United States, 43210 Austria Novartis Investigative Site Wien, Austria, A-1090 Belgium Novartis Investigative Site Leuven, Belgium, 3000 France Novartis Investigative Site Lyon, France, 69437 Novartis Investigative Site Villejuif Cedex, France, 94805 Germany Novartis Investigative Site Essen, Germany, 45147 Italy Novartis Investigative Site Firenze, FI, Italy, 50134 Novartis Investigative Site Milano, MI, Italy, 20133 Novartis Investigative Site Milano, MI, Italy, 20141 Netherlands Novartis Investigative Site Rotterdam, Netherlands, 3015 CE Spain Novartis Investigative Site Barcelona, Catalunya, Spain, 08035 Novartis Investigative Site Hospitalet de LLobregat, Catalunya, Spain, 08907 Novartis Investigative Site Madrid, Spain, 28041 United Kingdom Novartis Investigative Site Manchester, United Kingdom, M20 4BX 收起 <<
NCT01453595	-		Terminated(Given the number of... 展开 >> toxicities seen and the difficulty with patient retention in the dose escalation portion, the sponsor decided to close the trial.) 收起 <<	-	-
NCT01717898	Castrate-resistant Prostate Ca... 展开 >>ncer 收起 <<	Phase 1 Phase 2	Terminated(Dose limiting toxic... 展开 >>ities on lowest dose level) 收起 <<	-	United States, California ... 展开 >> University of California, San Francisco San Francisco, California, United States, 94115 收起 <<
NCT01658436	-		Completed	-	-
NCT01717898	-		Terminated(Dose limiting toxic... 展开 >>ities on lowest dose level) 收起 <<	-	-
NCT01856101	Carcinoma Transitional Cell	Phase 2	Terminated(Novartis decided to... 展开 >> stop the marketing of BEZ235) 收起 <<	-	Belgium ... 展开 >> Clinique Saint-Pierre à Ottignies Ottignies, Brabant Wallon, Belgium, 1340 Epicura- RHMS Baudour Baudour, Hainaut, Belgium, 7331 Grand Hôpital de Charleroi Charleroi, Hainaut, Belgium, 6000 Hôpital de Jolimont Haine-Saint-Paul, Hainaut, Belgium, 7100 Centre Hospitalier Wallonie Picarde Tournai, Hainaut, Belgium, 7500 CHU de Liège site du Sart Tilman Liège 1, Liège, Belgium, 4000 Clinique du Sud Luxembourg Arlon, Luxembourg, Belgium, 6700 CHU de Mont-Godinne Yvoir, Namur, Belgium, 5530 Cliniques universitaires Saint-Luc Brussel, Belgium, 1200 Universitair Ziekenhuis Gent Gent, Belgium, 9000 Clinique et Maternité Ste Elisabeth Namur, Belgium, 5000 Luxembourg Centre Hospitalier de Luxembourg Luxembourg, Grand-Duché de Luxembourg, Luxembourg, 1210 收起 <<
NCT01248494	Metastatic Breast Cancer	Phase 1	Completed	-	United States, Alabama ... 展开 >> University of Alabama Birmingham, Alabama, United States United States, Massachusetts Massachusetts General Hospital, Dana Farber Cancer Center Boston, Massachusetts, United States, 02114 United States, New York Columbia University Medical Center New York City, New York, United States United States, Tennessee Vanderbilt Cool Springs Nashville, Tennessee, United States, 37067 Vanderbilt Breast Center One Hundred Oaks Nashville, Tennessee, United States, 37204 Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232 收起 <<
NCT01343498	Malignant Solid Tumour	Phase 1	Completed	-	United States, Oklahoma ... 展开 >> Oklahoma University Oklahoma City, Oklahoma, United States, 71304 United States, Tennessee Tennessee Oncology Nashville, Tennessee, United States, 37203 收起 <<

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