PF-562271 HCl是PF-562271的盐酸盐形式，是一种强效的ATP竞争性的可逆的抑制剂，作用于FAK其IC50为1.5 nM。相比较FAK，对Pyk2的效果少了大约十倍，除了CDKs类的蛋白酶，PF-562271 HCl的选择性相比其他蛋白酶大大约100倍。 Information PF-562271 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor ofFAKwithIC50of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1. Targets FAK ; PYK2 ; CDK2/CyclinE ; CDK3/CyclinE ; CDK1/CyclinB 15161,1.5 nM; 13 nM; 30 nM; 47 nM; 58 nM In vitro PF-562271 binds in the ATP-binding cleft of FAK, forming two of the three “canonical” H-bonds between the inhibitor and main-chain atoms in the kinase hinge region. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM. PF-562271 (3.3 μM) results in G1 arrest of PC3-M cells. PF-562271 (1 nM) blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. PF-262271 potently blocks blood vessel sprouting without detectable changes in vascular leakage. PF-562271 (250 nM) results in complete inhibition of collective A431 cell invasion into collagen gels. In vivo PF-562271 (