Selective focal adhesion kinase (FAK) inhibitor that displays no significant activity at a range of other kinases including EGFR, PDGFR and IGF-RI. Prevents FAK autophosphorylation at Y397 (IC50 = 1 µM), promotes cell detachment and inhibits cell adhesion in vitro. Exhibits antiproliferative activity in a variety of human tumor cell lines in vitro and in breast cancer cells in vivo. Induces regression of pancreatic tumors2 and glioblastoma3. Displays antiangiogenic activity4.
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