PF-00477736
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 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.
Product Specifications
CAS Number
952021-60-2
Product Name Alternative
PF00477736 | PF-477736
Purity
>98% (HPLC)
Solubility
DMSO: 31.5 mg/mL (75 mM) (< 1 mg/ml refers to the product slightly soluble or insoluble)
Smiles
CN1C=C (C=N1) C2=C3C=NNC (=O) C4=C3C (=CC (=C4) NC (=O) C (C5CCCCC5) N) N2
Molecular Formula
C22H25N7O2
Molecular Weight
419.489
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
(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
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