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Description: PF-477736 di-HCl (also known as PF-736 diHCl, PF-00477736) is a novel, selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM in a cell-free assay and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes. It shows ca.100-fold selectivity for Chk1 than Chk2. By overriding the last checkpoint defense against DNA damaging agent-induced lethal damage, chk1 inhibitor PF-477736 may potentiate the antitumor efficacy of various chemotherapeutic agents against tumor cells with intrinsic checkpoint defects.
References: Mol Cancer Ther. 2008 Aug; 7(8):2394-404; Clin Cancer Res. 2009 Jul 15; 15(14):4630-40.
Related CAS: 952021-60-2 (free base); 1175132-90-7 (HCl); 1071848-28-6; 952238-93-6 (xHCl); 1247874-19-6 (2HCl)
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