PF-562271 besylate

F-562271 is an ATP-competitive, reversible inhibitor of FAK (IC₅₀ = 1.5 nM). It displays 10-fold reduced potency for PYK2 (IC₅₀ = 14 nM) and >100-fold selectivity against other protein kinases. PF-562271 inhibits FAK phosphorylation with an EC₅₀ value of 93 ng/ml in glioblastoma-bearing mice and has been shown to regress tumors in multiple xenograft models.