PI-103 | PI3K/mTOR Inhibitor | AmBeed-信号通路专用抑制剂

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PI-103 {[allProObj[0].p_purity_real_show]}

货号：A344838

PI-103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. It blocks autophagic flux.

PI-103 化学结构
CAS号：371935-74-9

PI-103 3D分子结构
CAS号：371935-74-9

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PI-103 纯度/质量文件产品仅供科研

货号：A344838 标准纯度： {[allProObj[0].p_purity_real_show]} 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, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

PI3K 亚型比较
自噬亚型比较
ATM/ATR 亚型比较
DNA-PK 亚型比较

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	98%
HS-173		++++ PI3Kα , IC50: 0.8 nM							99%+
Serabelisib		+++ PI3Kα, IC50: 21 nM							99%+
GNE-477		++++ PI3Kα, IC50: 4 nM						mTOR	98%
YM-201636		+ p110α, IC50: 3.3 μM						PIKfyve	98%
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					98+%
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			✔						98%
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				98+%
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				98%
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			98%
AS-605240		++ PI3Kα, IC50: 60 nM	+ PI3Kβ, IC50: 270 nM	+++ PI3Kγ, IC50: 8 nM	+ PI3Kδ, IC50: 300 nM				98%
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	98+%
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				98+%
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	98%+
CZC24832			+ PI3Kβ, IC50: 1.1 μM	++ PI3Kγ, IC50: 27 nM					98+%
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				98%+
PI3K-IN-1		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	98+%
TG100-115		+ PI3Kα, IC50: 1.3 μM	+ PI3Kβ, IC50: 1.2 μM	++ PI3Kγ, IC50: 83 nM	+ PI3Kδ, IC50: 235 nM				98%
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				95%
Quercetin			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM			Sirtuin,Src,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			✔						98%
Eganelisib				+++ PI3Kγ, IC50: 16 nM					99%+
CAY10505				✔					98%
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				95+%
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				98%
PI3Kδ-IN-5					++++ PI3Kδ, IC50: 0.9 nM				98%
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		DNA-PK,MLCK	99%+
Samotolisib						✔		DNA-PK	99%+
GNE-317						✔			99%+
Oroxin B						✔		PTEN,Akt	99%+
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	98+%
Deguelin						✔		Akt	99%+
Ailanthone						✔		ATM/ATR,CDK,Akt	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	98%
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		98+%
3-Methyladenine				+ PI3Kγ, IC50: 60 μM			+ Vps34, IC50: 25 μM	Autophagy	98%
Vps34-IN-4							+++ VPS34, IC50: 15 nM		98%+
Autophinib							+++ Vps34, IC50: 19 nM	Autophagy	97%
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	Autophagy ↓ ↑	其他靶点	纯度
SBI-0206965	+++ ULK1, IC50: 108 nM ULK2, IC50: 711 nM		97%
Hydroxychloroquine sulfate	✔		99%
Valproic acid sodium	✔	HDAC	97%
PFK-015	++ PFKFB3, IC50: 207 nM		99%+
MRT68921 hydrochloride	++++ ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM		99%+
ROC-325	✔		99%+
Autophinib	+++ Autophagy, IC50: 40 nM		97%
Lys05	✔		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		PI3K,DNA-PK,MLCK	99%+
CP-466722	+ ATM, IC50: 410 nM			99%+
Torin 2	++ ATM, EC50: 28 nM	++ ATR, EC50: 35 nM	DNA-PK,mTOR	99%+
KU-55933	+++ ATM, IC50: 12.9 nM			96%
ETP-46464	+ ATM, IC50: 545 nM	+++ ATR, IC50: 14 nM	DNA-PK,mTOR	98%
CGK733	++ ATM, IC50: 200 nM	++ ATR, IC50: 200 nM		99%+
AZD0156	✔			99%+
Dactolisib		+++ ATR, IC50: 21 nM		98+%
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	98%
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	DNA-PK ↓ ↑	其他靶点	纯度
PI-103	++ DNA-PK, IC50: 23 nM		99%+
CC-115	+++ DNA-PK, IC50: 0.013 μM	mTOR	98+%
Samotolisib	✔		99%+
NU 7026	+ DNA-PK, IC50: 0.23 μM	PI3K	98+%
PIK-75 HCl	++++ DNA-PK, IC50: 2 nM		99%+
PP121	+ DNA-PK, IC50: 60 nM	PDGFR,VEGFR	99%+
KU-0060648	++++ DNA-PK, IC50: 5 nM		99%
KU-57788	+++ DNA-PK, IC50: 14 nM		99%+
LTURM34	++ DNA-PK, IC50: 0.034 μM		98%+
SF2523	+++ DNA-PK, IC50: 9 nM		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。

PI-103 生物活性

靶点	p110γ p110γ, IC50:15 nM p110β p110β, IC50:3 nM p110α p110α, IC50:2 nM p110δ p110δ, IC50:3 nM
描述	PI3K/AKT/mTOR pathway directly relates to cellular quiescence, proliferation, cancer, and longevity. There are eight PI3 kinases have been identified as classes IA, 1B, II, and III based on the sequence homology and substrate preference. Among them, class IA PI3K is composed of a heterodimer consisting of a 110 kDa catalytic subunit (p110α, p110β and p110δ) and an 85 kDa regulatory subunit ^[2]. PI-103 is a dual inhibitor of Class IA PI3Ks (p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM determined using a scintillation proximity assay, respectively) and mTOR (IC50=30 nM), with less potent to DNA-PK (IC50=23 nM) ^[1]. PI-103 is usually used in ACUTE LYMPHOBLASTIC LEUKEMIA study. It can inhibit PI3K/Akt and mTORC1 activity in MOLM14, OCI-AML3 and MV4-11 leukemic cell lines, which have constitutive activation of PI3K/Akt (p-Akt Ser 473 and p-FOXO3a Thr32), mTORC1 (p-P70S6K Thr389) signaling pathways, with no inhibition on ERK/MAPK (p-p42/44 ERK/MAPK Thr202/Tyr204). In AML blast cells, PI-103 inhibits both constitutive and growth factor-induced PI3K/Akt and mTORC1 activation, reverses the positive feedback of mTORC1 inhibition on PI3K/Akt and induces significant apoptosis ^[3]. In glioma, PI‑103 induces autophagy and promotes cell survival by inhibiting mTOR activity. Conversely, PI‑103 can lead to apoptosis by combining with autophagy inhibitors like 3-ma or bafilomycin A1 ^[4].
作用机制	PI-103 acts as an ATP-competitive inhibitor of PI3K (Class IA). ^[5]

PI-103 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
518A2	0.01–10 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	21048785
518A2	0.001–1 μM	Function Assay	24 h	suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets	21048785
A549	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation slightly	24351425
A549	0-3.3 μM	Function Assay	72 h	induces complete downregulation of pAKT	23259591

PI-103 动物研究

Dose	Mice: min = 5 mg/kg^[5] Nude Mice: min = 30 mg/kg, max = 100 mg/kg^[6]
Administration	i.p.

PI-103 参考文献

[1]Raynaud FI, Eccles SA, et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Mol Cancer Ther. 2009 Jul;8(7):1725-38.

[2]Zhao HF, Wang J, et al. Recent advances in the use of PI3K inhibitors for glioblastoma multiforme: current preclinical and clinical development. Mol Cancer. 2017 Jun 7;16(1):100.

[3]Park S, Chapuis N, et al. PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML. Leukemia. 2008 Sep;22(9):1698-706.

[4]Fan QW, Weiss WA, et al. Autophagy and Akt promote survival in glioma. Autophagy. 2011 May;7(5):536-8. Epub 2011 May 1.

PI-103 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.35mL

2.87mL

1.44mL

28.71mL

5.74mL

2.87mL

PI-103 技术信息

CAS号	371935-74-9
分子式	C₁₉H₁₆N₄O₃
分子量	348.355

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 9 mg/mL(25.84 mM)，配合低频超声助溶，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

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 60 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

518A2	0.01–10 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	21048785
518A2	0.001–1 μM	Function Assay	24 h	suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets	21048785
A549	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation slightly	24351425
A549	0-3.3 μM	Function Assay	72 h	induces complete downregulation of pAKT	23259591
AGS HG		Growth Inhibition Assay		IC50=0.68 ± 0.031 μM	24597478
AGS LG		Growth Inhibition Assay		IC50=0.05 ± 0.001 μM	24597478
ALL-SIL	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
BT549	0-3 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25721419
CCRF-CEM	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
DETROIT562		Growth Inhibition Assay		IC50=0.13 μM	19584227
DND41	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
FaDu	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation significantly	24351425
G 35 DC	0.05-20 μM	Growth Inhibition Assay	24/72 h	inhibits cell viability dose and time dependently	26121251
G 35 SC	0.05-20 μM	Growth Inhibition Assay	24/72 h	inhibits cell viability dose and time dependently	26121251
G 38 DC	0.05-20 μM	Growth Inhibition Assay	24/72 h	inhibits cell viability dose and time dependently	26121251
G 38 SC	0.05-20 μM	Growth Inhibition Assay	24/72 h	inhibits cell viability dose and time dependently	26121251
G 40 DC	0.05-20 μM	Growth Inhibition Assay	24/72 h	inhibits cell viability dose and time dependently	26121251
G 40 SC	0.05-20 μM	Growth Inhibition Assay	24/72 h	inhibits cell viability dose and time dependently	26121251
H3122	0-3.3 μM	Function Assay	72 h	induces complete downregulation of pAKT	23259591
H460	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation slightly	24351425
H661	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation significantly	24351425
HCC1937	1 μM	Function Assay	24 h	reduces the phosphorylation of AKT	22488590
HCC827	0-3.3 μM	Function Assay	72 h	induces complete downregulation of pAKT	23259591
HCC827	0-3 μM	Growth Inhibition Assay	72 h	IC50=0.3 μM	21220474
HGC27 HG		Growth Inhibition Assay		IC50=0.38 ± 0.022 μM	24597478
HGC27 LG		Growth Inhibition Assay		IC50=0.02 ± 0.004 μM	24597478
HPB-ALL	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
HS578T	0-3 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25721419
HS578T	0.01-10 μM	Function Assay	24 h	downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins	25721419
HT1080	3 µM	Apoptosis Assay	12 h	sensitizes RD cells to DOX-induced apoptosis	23300809
HUVEC		Growth Inhibition Assay		IC50=0.08 μM	19584227
IGROV-1		Growth Inhibition Assay		IC50=0.06 μM	19584227
Jurkat	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
Karpas-45	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
KE37	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
KMS12-BM	0-2 μM	Growth Inhibition Assay	24 h	IC50＞2 μM	22829234
LN229	1 μM	Function Assay	48 h	induces autophagosome formation	21062993
LOUCY	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
MDA-MB-231	0-3 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25721419
MDA-MB-231	0.01-10 μM	Function Assay	24 h	downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins	25721419
MDA-MB-231	0.3 μM	Cell Viability Assay	72 h	enhances cytotoxic effects of PI3K/AKT pathway inhibitors	23601074
MDA-MB-436	0-3 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25721419
MDA-MB-436	1 μM	Function Assay	24 h	reduces the phosphorylation of AKT	22488590
MDA-MB-468	0-3 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25721419
MDA-MB-468	0.01-10 μM	Function Assay	24 h	downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins	25721419
MDA-MB-468	0.3 μM	Cell Viability Assay	72 h	enhances cytotoxic effects of PI3K/AKT pathway inhibitors	23601074
Mel-Juso	0.01–10 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	21048785
Mel-Juso	0.001–1 μM	Function Assay	24 h	suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets	21048785
MKN45 HG		Growth Inhibition Assay		IC50=1.01 ± 0.051 μM	24597478
MKN45 LG		Growth Inhibition Assay		IC50=0.87 ± 0.030 μM	24597478
MM1S	0-2 μM	Growth Inhibition Assay	24 h	IC50=0.5 μM	22829234
MOLT-16	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
MOLT-4	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
NCI-H929	0-2 μM	Growth Inhibition Assay	24 h	IC50=0.25 μM	22829234
NUGC4 HG		Growth Inhibition Assay		IC50=14.0 ± 3.913 μM	24597478
NUGC4 LG		Growth Inhibition Assay		IC50=14.0 ± 5.321 μM	24597478
PC3		Growth Inhibition Assay	24h	GI50 = 100 nM	20551061
PC3		Growth Inhibition Assay		IC50=0.10 μM	19584227
PC-9	0-3 μM	Growth Inhibition Assay	72 h	IC50=0.8 μM	21220474
PEER	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
PF-382	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
RD	1/1.5/2 μM	Apoptosis Assay	72 h	induces apoptosis combined with GANT61	25749378
RD	1/1.5/2 μM	Apoptosis Assay	72 h	induces caspase-dependent apoptosis combined with UO126	23684925
RD	3 µM	Apoptosis Assay	12 h	sensitizes RD cells to DOX-induced apoptosis	23300809
RH30	1/1.5/2 μM	Apoptosis Assay	72 h	induces apoptosis combined with GANT61	25749378
RH30	1/1.5/2 μM	Apoptosis Assay	72 h	induces caspase-dependent apoptosis combined with UO126	23684925
RMS13	1/1.5/2 μM	Apoptosis Assay	72 h	induces apoptosis combined with GANT61	25749378
RMS13	1/1.5/2 μM	Apoptosis Assay	72 h	induces caspase-dependent apoptosis combined with UO126	23684925
RPMI-8402	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
SAS	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation significantly	24351425
SF767	1 μM	Function Assay	48 h	induces autophagosome formation	21062993
SH-SY5Y	0-8 μM	Growth Inhibition Assay	24/48/72 h	induces time- and concentration-dependent inhibition on NB cell growth	26224681
SH-SY5Y	1 μM	Apoptosis Assay	0.5-24 h	sensitizes neuroblastoma cells to doxorubicin-induced apoptosis	26224681
SK-N-BE	0-8 μM	Growth Inhibition Assay	24/48/72 h	induces time- and concentration-dependent inhibition on NB cell growth	26224681
SKNBE(2c)	1.5/2.5/5 μM	Function Assay	24 h	induces G1 cell-cycle arrest and apoptosis	23378341
SKOV-3		Growth Inhibition Assay		IC50=0.12 μM	19584227
SUM1315MO2	1 μM	Function Assay	24 h	reduces the phosphorylation of AKT	22488590
SUM149PT	0-3 μM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	25721419
SUM149PT	0.3 μM	Cell Viability Assay	72 h	enhances cytotoxic effects of PI3K/AKT pathway inhibitors	23601074
SUM149PT	1 μM	Function Assay	24 h	reduces the phosphorylation of AKT	22488590
SUP-T1	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
SW872	0.01-0.5 μM	Function Assay	24 h	reduces AKT phosphorylation (pAKT) and 4EBP1 phosphorylation (p4EBP1) in a dose-dependent manner	24695632
SW872	0.01-0.5 μM	Apoptosis Assay	48 h	induces apoptosis dose dependently	24695632
SW982	0.01-0.5 μM	Function Assay	24 h	reduces AKT phosphorylation (pAKT) and 4EBP1 phosphorylation (p4EBP1) in a dose-dependent manner	24695632
SW982	0.01-0.5 μM	Apoptosis Assay	48 h	induces apoptosis dose dependently	24695632
SY5Y	1.5/2.5/5 μM	Function Assay	24 h	induces G1 cell-cycle arrest and apoptosis	23378341
TALL-1	1 μM	Growth Inhibition Assay	7 d	decreases the cell number significantly	23038273
TE381.T	1/1.5/2 μM	Apoptosis Assay	72 h	induces apoptosis combined with GANT61	25749378
TE671	1/1.5/2 μM	Apoptosis Assay	72 h	induces caspase-dependent apoptosis combined with UO126	23684925
TP5014	3 µM	Apoptosis Assay	12 h	sensitizes RD cells to DOX-induced apoptosis	23300809
U118MG	0.1-1 μM	Function Assay	24 h	inhibits PI3K-mediated signaling	19633683
U138MG	0.1-1 μM	Function Assay	24 h	inhibits PI3K-mediated signaling	19633683
U373	1 μM	Function Assay	48 h	induces autophagosome formation	21062993
U87	1 μM	Function Assay	48 h	induces autophagosome formation	21062993
U87MG	0.1-1 μM	Function Assay	24 h	inhibits PI3K-mediated signaling	19633683
U87MG		Growth Inhibition Assay		IC50=0.14 μM	19584227
UCH-1	0-5 μM	Function Assay		inhibits the phosphorylation of both AKT and mTOR in a dose-dependent manner	19528441
UCH-1	0.01-10 μM	Growth Inhibition Assay	6 d	inhibits proliferation dose dependently	19528441
UCH-1	0.1-10 μM	Apoptosis Assay	24 h	induces apoptosis	19528441
UT5	0.25/0.5/1 μM	Function Assay	24 h	inhibits Akt phosphorylation significantly	24351425
VJ	1/1.5/2 μM	Apoptosis Assay	72 h	induces apoptosis combined with GANT61	25749378

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p110γ	p110γ, IC50:15 nM
p110β	p110β, IC50:3 nM
p110α	p110α, IC50:2 nM
p110δ	p110δ, IC50:3 nM
mTOR	mTOR, IC50:30 nM
DNA-PK	DNA-PK, IC50:23 nM

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