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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Checkpoint Kinase (Chk)-PF-00477736
PF-00477736

Chemical Structure : PF-00477736

CAS No.: 952021-60-2

PF-00477736 (PF00477736;PF-477736)

货号: PC-35602Not For Human Use, Lab Use Only.

PF-00477736 (PF-477736) is a potent, selective, ATP-competitive inhibitor of Chk1 with Ki of 0.49 nM, also inhibits Chk2 (Ki=47 nM) and poorly inhibits CDK1 activity (Ki=9.9 uM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PF-00477736 (PF-477736) is a potent, selective, ATP-competitive inhibitor of Chk1 with Ki of 0.49 nM, also inhibits Chk2 (Ki=47 nM) and poorly inhibits CDK1 activity (Ki=9.9 uM).
PF-00477736 displays <100-fold selectivity over VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret, and Yes in a panel of >100 protein kinases.
PF-00477736 abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin; enhances the antitumor activity of gemcitabine in a dose-dependent manner in xenografts.

物理化学性质&存储条件

分子量 419.489
分子式 C22H25N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-2-amino-2-cyclohexyl-N-(5-(1-methyl-1H-pyrazol-4-yl)-1-oxo-2,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-yl)acetamide

参考文献

1. Blasina A, et al. Mol Cancer Ther. 2008 Aug;7(8):2394-404.

2. Zhang C, et al. Clin Cancer Res. 2009 Jul 15;15(14):4630-40.

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