REVIEW PF-562,271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 catalytic activity with a IC50 of 1.5 and 14 nmol/L, respectively (PMID 18339875). In addition, PF-562,271. PF-562,271 displayed robust inhibition in an inducible cell-based assay measuring phospho-FAK with an IC(50) of 5 nmol/L. PF-562,271 was evaluated against multiple kinases and displays >100x selectivity against a long list of nontarget kinases. In tests, PF-562,271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion with a calculated EC50 of 93 ng/mL using injections.
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