Cabozantinib
Met and VEGFR2 inhibitor / Novel inhibitor of c-met and VEGFR2 kinase activity, IC50=3.5 nm and 35 pM respectively.1 Inhibits MET-activating kinase domain mutations Y1248H, D1246N or K1262R, IC50=3.8, 11.8 and 14.6 nM respectively. In cellular assays it inhibits the following kinases: MET, VEGF2, KIT, FLT3 and AXL, IC50=7.8, 1.9, 5.0, 7.5 and 42 μM respectively.1 Eliminated approximately 80% of vasculature in spontaneous pancreatic islet tumors over 7 days in a mouse model.2 Clinically useful anticancer agent.3
Biochemicals & reagents
849217-68-1
XL-184; BMS-907351;
1) Yakes et al. (2011), Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth; Mol. Cancer Ther., 10 2298 2) You et al. (2011), VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer; Cancer Res., 71 4758 3) Kurzrock et al. (2011), Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor in patients with medullary thyroid cancer; J. Clin. Oncol., 29 2660
-20°C
TARGET: Kinase -- DISEASE AREA: Cancer