Potent inhibitor of VEGFR-2, -3, and -1, IC50 = 0.2, 0.1-0.3, and 1.2 nM respectively displaying minimal activity against a panel of ~100 protein kinases. Inhibits angiogenesis and vascular permeability. Also inhibits BCR-ABL1 (T315I) with high potency, Ki = 149 pM for autophosphorylated ABL1 (T315I). Inhibits proliferation of Ba/F3 cells expressing BCR-ABL1 (T315I). Clinically useful anticancer agent.
Application Procedures
First dissolved in DMSO (up to 30 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.
