The cytoplasmic protein-tyrosine kinase FAK is associated with integrins and growth factor receptors. It modulates a variety of cellular processes when it is activated. Since the elevated expression of FAK is found in many tumors, the inhibitors of FAK are developed as anti-tumor drugs in cancer therapy. PND-1186 is one of these ATP-competitive small-molecule inhibitors. It inhibited the autophosphorylation of FAK tyrosine-397 with IC50 value of 0.1 μM in breast carcinoma cells. When the concentration was up to 1 μM, PND-1186 also inhibited more than 50% of the activities of other kinases, such as CDK2, Lck, Aurora-A and ACK1
产品描述
PND-1186 is a reversible inhibitor of FAK (focal adhesion kinase) with IC50 value of 1.5 nM
