PF-00477736

Research use only, not for human use.

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 (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); displays <100-fold selectivity over VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret, and Yes in a panel of >100 protein kinases; 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.Solid Tumors Phase 1 Discontinued.

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PF00477736 | PF-477736

Angiogenesis

Chk

c-Fms|Chk1|Chk2|VEGFR2|Yes

Cancer

Solid Tumors

952021-60-2

419.489

C22H25N7O2

>98% (HPLC)

DMSO: 31.5 mg/mL (75 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

CN1C=C(C=N1)C2=C3C=NNC(=O)C4=C3C(=CC(=C4)NC(=O)C(C5CCCCC5)N)N2

(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

(-20℃)

With Ice Pack

≥ 2 years