Orally active receptor tyrosine kinase inhibitor against VEGFR (Flt-1/KDR/Flt-4), PDGFR1/2, and KIT with anti-angiogenesis efficacy in vitro and in vivo.

Pazopanib is an orally active receptor tyrosine kinases inhibitor against VEGFR1/2/3 (IC50 = 10/30/47 nM), PDGFR1/2 (IC50 = 84/71 nM) and c-Kit (IC50 = 74 nM), exhibiting reduced or no potency toward FGFR1/3 (IC50 = 140/130 nM), c-fms (IC50 = 146 nM), and other kinases tested (IC50 from >400 nM to >20 μM). Pazopanib exhibits anti-cancer efficacy in cultures (IC50 from 5 to 15 μg/mL; multiple myeloma migration and survival) and in mice in vivo (30-100 mg/kg/day p.o. against human MM xenografts) via angiogenesis inhibition and apoptosis induction.