PF-562271

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 displayed robust inhibition in an inducible cell-based assay measuring phospho-FAK with an IC₅₀ 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.

Focal Adhesion Kinase (FAK) is a protein coded by the PTK2 gene that plays an essential role in regulating cell migration, adhesion, spreading, reorganization of the actin cytoskeleton, formation and disassembly of focal adhesions and cell protrusions, cell cycle progression, cell proliferation and apoptosis.