PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1 , with a K i of 0.49 nM, it is also a Chk2 inhibitor, with a K i of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2 , Fms , Yes , Aurora-A , FGFR3 , Flt3 , and Ret ( IC 50 =8 (K i ), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.
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