PF-562271 is a reversible, ATP-competitive inhibitor of focal adhesion kinase (FAK) and Pyk2 with an IC50 of 1.5 and 14 nM, respectively. [1] In an inducible cell-based assay measuring phospho-FAK, it robustly inhibits at an IC50 of 5 nM. In vivo, PF-562271 inhibits FAK phosphorylation in a dose-dependent fashion at an EC50 of 93 ng/mL.

PF-562271 has been evaluated as a potential therapy for pancreatic ductal adenocarcinoma [2] and for cancer patients with bone metastases and cancer-associated osteoporosis. [3]

PF-562271 has been studied in combination with gemcitabine in pancreatic cancers, and sunitinib in hepatocellular carcinomas. [4] In the sunitinib / PF-562271 combination studies, both angiogenesis and tumor proliferation were addressed, posing a formidable approach to treating solid tumors of the liver.