AV-951 is an potent and selective orally bioavailable isoxazole inhibitor of VEGFR1, 2, and 3, kinases at 0.21, 0.16, and 0.24 nM, respectively. Additionally it has nanomolar activity for cKIT and PDGFR at 1.63 and 1.72 nM, respectively. [1] In vitro, AV-951 blocks MAP kinase activation and suppresses the proliferation and migration of endothelial cells. In vivo, it suppresses angiogenesis and tumor progression in human xenografts. [2]

AV-951 has been widely studied in clinical trials for the treatment of advanced renal cell carcinoma (RCC) and non-small cell lung cancers (NSCLC). More recent studies are exploring combination therapies with paclitaxel and bevacizumab for breast and colorectal cancer, respectively.

AV-951 is an potent and selective orally bioavailable isoxazole inhibitor of VEGFR1, 2, and 3, kinases at 0.21, 0.16, and 0.24 nM, respectively. Additionally it has nanomolar activity for cKIT and PDGFR at 1.63 and 1.72 nM, respectively. [1] In vitro, AV-951 blocks MAP kinase activation and suppresses the proliferation and migration of endothelial cells. In vivo, it suppresses angiogenesis and tumor progression in human xenografts. [2]

AV-951 has been widely studied in clinical trials for the treatment of advanced renal cell carcinoma (RCC) and non-small cell lung cancers (NSCLC). More recent studies are exploring combination therapies with paclitaxel and bevacizumab for breast and colorectal cancer, respectively.