Danusertib | PHA-739358 | Aurora Kinase Inhibitor | AmBeed-信号通路专用抑制剂

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达鲁舍替 /Danusertib {[allProObj[0].p_purity_real_show]}

货号：A395008 同义名： PHA-739358

Danusertib is a pyrrolo-pyrazole and small molecule Aurora kinases inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively. It is modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc.

Danusertib 化学结构
CAS号：827318-97-8

Danusertib 3D分子结构
CAS号：827318-97-8

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Danusertib 纯度/质量文件产品仅供科研

货号：A395008 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

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Aurora Kinase 亚型比较
转化生长因子-β 亚型比较
Bcr-Abl 亚型比较
c-RET 亚型比较

产品名称	Aurora A ↓ ↑	Aurora B ↓ ↑	Aurora C ↓ ↑	其他靶点	纯度
BI-847325	++ Aurora A (Human), IC50: 25 nM	++++ Aurora B (Xenopus laevis), IC50: 3 nM	++ Aurora C (Human), IC50: 15 nM		99%+
CCT 137690	++ Aurora A, IC50: 15 nM	++ Aurora B, IC50: 25 nM	++ Aurora C, IC50: 19 nM		99%+
MK-5108	++++ Aurora A, IC50: 0.064 nM				99%+
KW-2449	+ Aurora A, IC50: 48 nM			FLT3	99%+
Tozasertib	++++ Aurora A, Ki app: 0.6 nM	++ Aurora B, Ki app: 18 nM	+++ Aurora C, Ki app: 4.6 nM	FLT3,Bcr-Abl	99%+
AT9283	++++ Aurora A, IC50: ~3.0 nM	++++ Aurora B, IC50: ~3.0 nM			99%+
MLN8054	+++ Aurora A, IC50: 4 nM	+ Aurora B, IC50: 172 nM			99%+
ZM-447439	+ Aurora A, IC50: 110 nM	+ Aurora B, IC50: 130 nM		Src	99%+
TCS7010	++++ Aurora A, IC50: 3.4 nM				99%+
TAK-901	++ Aurora A-TPX2, IC50: 21 nM	++ Aurora B-INCENP, IC50: 15 nM			99%+
Danusertib	+++ Aurora A, IC50: 13 nM	+ Aurora B, IC50: 79 nM	+ Aurora C, IC50: 61 nM	RET	99%+
MK-8745	++++ Aurora A, IC50: 0.6 nM				99+%
PHA-680632	++ Aurora A, IC50: 27 nM	+ Aurora B, IC50: 135 nM	+ Aurora C, IC50: 120 nM	FLT3	99%+
AMG 900	+++ Aurora A, IC50: 5 nM	+++ Aurora B, IC50: 4 nM	++++ Aurora C, IC50: 1 nM		99%+
Alisertib	++++ Aurora A, IC50: 1.2 nM				99%+
ENMD-2076	+++ Aurora A, IC50: 14 nM	+ Aurora B, IC50: 350 nM		FLT3,RET	98%
JNJ-7706621	+++ Aurora A, IC50: 11 nM	++ Aurora B, IC50: 15 nM			99%+
CYC-116	+++ Aurora A, Ki: 8 nM	+++ Aurora B, Ki: 9 nM		FLT3	99%+
Reversine	+++ Aurora A, IC50: 12 nM	+++ Aurora B, IC50: 13 nM	++ Aurora C, IC50: 20 nM		98%
CCT129202	++ Aurora A, IC50: 42 nM	+ Aurora B, IC50: 198 nM	+ Aurora C, IC50: 227 nM		98%
SNS-314 mesylate	+++ Aurora A, IC50: 9 nM	++ Aurora B, IC50: 31 nM	++++ Aurora C, IC50: 3 nM		99%+
Barasertib-HQPA		++++ Aurora B, IC50: 0.37 nM			99%+
Hesperadin		+ Aurora B (human), IC50: 250 nM			98%
GSK-1070916		++++ Aurora B-INCENP, IC50: 3.5 nM	+++ Aurora C-INCENP, IC50: 6.5 nM	SIK,Tie-2	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	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		98%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 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。

产品名称	Abl ↓ ↑	Bcr-Abl ↓ ↑	其他靶点	纯度
NVP-BHG 712	+ c-Abl, IC50: 1.667 μM			99%+
KW-2449	+++ Abl, IC50: 14 nM Abl (T315I), IC50: 4 nM		FLT3	99%+
Ponatinib	++++ Abl, IC50: 0.37 nM			98%
AT9283				99%+
Imatinib Mesylate	+ v-Abl, IC50: 600 nM		c-Kit,PDGFR	99%
Danusertib	++ Abl, IC50: 25 nM		RET	99%+
Rebastinib	++++ p-Abl1 (native), IC50: 0.75 nM u-Abl1 (T315I), IC50: 5 nM		FLT3,Tie-2	99%+
PP121	++ Abl, IC50: 18 nM		PDGFR,VEGFR	99%+
GNF-7	+++ M351T, IC50: 133 nM E255V, IC50: 122 nM			99%+
Olverembatinib dimesylate	++++ Abl, IC50: 0.34 nM Abl (G250E), IC50: 0.35 nM			99%
Dasatinib monohydrate	++++ Abl , IC50: 0.6 nM		Src	98%
Dasatinib	++++ Abl, IC50: 0.6 nM		Src	98%
Bafetinib	+++ Abl, IC50: 5.8 nM			98+%
GNF-2		+ Bcr-Abl (SUP-B15 cell line), IC50: 268 nM Bcr-Abl (K562 cell line), IC50: 273 nM		98%+
Degrasyn		+ Bcr-Abl, IC50: 1.8 μM	DUB	98+%
GNF-5		++ Bcr-Abl, IC50: 220 nM		98%
Radotinib		++ BCR-ABL1, IC50: 34 nM		98+%
PD173955			Src	99%+
Nilotinib		++ Bcr-Abl, IC50: <30 nM		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	c-RET ↓ ↑	其他靶点	纯度
Regorafenib	+++ RET, IC50: 1.5 nM		98%
TG101209	++ RET, IC50: 17 nM	FLT3	99%+
Danusertib	+ RET, IC50: 31 nM		99%+
AD80	++++ RET V804M, IC50: 0.6 nM RET wt, IC50: 1.3 nM	Src,Raf	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。

Danusertib 生物活性

靶点	Aurora A Aurora A, IC50:13 nM Aurora B Aurora B, IC50:79 nM Aurora C Aurora C, IC50:61 nM FGFR1 FGFR1, IC50:47 nM
描述	The Aurora family of serine/threonine kinases, which consists of Aurora A, B and C, plays an important role in chromosome alignment, segregation, and cytokinesis during mitosis. Danusertib is pan-Aurora inhibitor with IC50 values of 13, 79, and 61 nM for Aurora A, B, and C (measured by in vitro kinase assays), respectively, also shows inhibitory effect on Abl, TrkA, c-RET and FGFR1 with IC50 values of 25nM, 31nM, 31nM and 47nM, respectively. Treatment with Danusertib below 10μM inhibited autophosphorylation in position Thr288 of Aurora A and histone H3 in position Ser10, the substrate of Aurora B, suggesting the cellular inhibition on Aurora A and Aurora B kinase activity by Danusertib in HeLa cells. Consistent with the in vitro kinase assays, the inhibition on c-RET, TrkA and FGFR1 by Danusertib can be observed, performing by the decreased pRet-Y905 in TT cells, decreased pTrkA-Y490 induced by NGF in PC-12 cells and decreased pERK1/2 of FGFR1 downstream induced by FGF not EGF in NIH-3T3 cells. Danusertib showed widely antiproliferative effect with IC50 values ranging in 28-300nM in several tumor cell lines covering different histotypes, including colon, breast, prostate, lung, and ovary. This anti-proliferation by Danusertib may due to both inhibition of Aurora B and defects of the p53-p21–dependent postmitotic checkpoint, and these markers can also be observed in in vivo study. Administration of Danusertib at dose of 25-30 mg/kg, i.v., bd, showed antitumor activity in several human tumor xenograft models, including HL-60, A2780, HCT-116, DMBA-induced mammary carcinoma, MMTV-RAS transgenic mammary carcinoma and TRAMP transgenic prostate carcinoma^[1].
作用机制	Danusertib is a small molecule ATP competitive pan-aurora kinase inhibitor.^[2]

Danusertib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A2780 cells		Proliferation assay		Antiproliferative activity against A2780 cells, IC50=28 nM	17125279
HCT116 cells		Proliferation assay		Antiproliferative activity against HCT116 cells, IC50=31 nM	17125279
HCT116 cells		Function assay		Cell cycle arrest in HCT116 cells by accumulation at G2/M phase, EC50=80 nM	17125279
HCT116 cells		Function assay		Inhibition of histone h3 phosphorylation in HCT116 cells by Western blot analysis	17125279

Danusertib 动物研究

Dose	Mice: 15 mg/kg^[3] (i.p.), 100 mg/kg^[3] (p.o.)
Administration	i.p., p.o.

Danusertib 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
NCT00335868	Leukemia	Phase 2	Unknown	-	United States, California ... 展开 >> Jonsson Comprehensive Cancer Center at UCLA Los Angeles, California, United States, 90095-1781 收起 <<
NCT00766324	Metastatic Hormone Refractory ... 展开 >>Prostate Cancer 收起 <<	Phase 2	Completed	-	Italy ... 展开 >> Nerviano Medical Sciences. Clinical Research Dept. Nerviano, Milano, Italy, 20014 收起 <<
NCT00872300	Multiple Myeloma	Phase 2	Terminated(Low recruitment rat... 展开 >>e) 收起 <<	-	United States, Arizona ... 展开 >> MAYO Clinic Scottsdale, Arizona, United States, 85259 United States, Illinois The Robert H Lurie Comprehensive Cancer Center, Northwestern University Chicago, Illinois, United States, 60611 France Hôpital Huriez, Centre Hospitalier Régional Universitaire de Lille Lille, France, 59037 University Hospital Hôtel-Dieu Nantes, France, 44093 收起 <<

Danusertib 参考文献

[1]Carpinelli P, Ceruti R, et al. PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3158-68.

[2]Borthakur G, Dombret H, et al. A phase I study of danusertib (PHA-739358) in adult patients with accelerated or blastic phase chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia resistant or intolerant to imatinib and/or other second generation c-ABL therapy. Haematologica. 2015 Jul;100(7):898-904.

Danusertib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.54mL

2.11mL

1.05mL

21.07mL

4.21mL

2.11mL

Danusertib 技术信息

CAS号	827318-97-8
分子式	C₂₆H₃₀N₆O₃
分子量	474.555

别名	PHA-739358
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

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

溶解度

DMSO: 50 mg/mL(105.36 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

达鲁舍替 /Danusertib {[allProObj[0].p_purity_real_show]}

Danusertib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Danusertib 质控信息

Danusertib 生物活性

Danusertib 细胞研究

Danusertib 动物研究

Danusertib 临床研究

Danusertib 参考文献

Danusertib 实验方案

Danusertib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

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热门区域

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Aurora A	Aurora A, IC50:13 nM
Aurora B	Aurora B, IC50:79 nM
Aurora C	Aurora C, IC50:61 nM
FGFR1	FGFR1, IC50:47 nM
Abl	Abl, IC50:25 nM
c-RET	RET, IC50:31 nM

达鲁舍替 /Danusertib {[allProObj[0].p_purity_real_show]}

Danusertib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Danusertib 质控信息

Danusertib 生物活性

Danusertib 细胞研究

Danusertib 动物研究

Danusertib 临床研究

Danusertib 参考文献

Danusertib 实验方案

Danusertib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Danusertib 纯度/质量文件产品仅供科研