Pazopanib
Multi-receptor tyrosine kinase inhibitor / Inhibits multiple receptor tyrosine kinases including VEGFR1,2 and 3 (IC50s=10, 30, 47 nM respectively) and PDGFRα, β and c-Kit (IC50s=71, 84, 74 nM respectively) and others such as FGFR.1 The drug targets both the tumor and endothelial cells in a mouse xenograft model of human multiple myeloma.2 It reduces joint pain and inhibits cartilage degeneration in rodent osteoarthritis models.3 VEGF inhibitors such as pazopanib have potential for treatment of neovascular age-related macular degeneration.4 In clinical use for renal cell carcinoma.5
Biochemicals & reagents
444731-52-6
GSK-VEG10003; GW786034B
1 Kumar et al. (2007) Pharmacokinetic-pharmacodynamic correlation from mouse to human with pazopanib, a multikinase angiogenesis inhibitor with potent antitumor and antiangiogenic activity; Mol. Cancer Ther. 6 2012 2 Podar et al. (2006) The small-molecule VEGF receptor inhibitor pazopanib (GW786034B) targets both tumor and endothelial cells in multiple myeloma; Proc. Natl. Acad. Sci. USA 103 19478 3 Ma et al. (2023) Targeting Vascular Endothelial Growth Factor Receptors as a Therapeutic Strategy for Osteoarthritis and Associated Pain; Int. J. Biol. Sci. 19 675 4 Rami-Baraka and Kaiser (2009) VEGF inhibitors for the treatment of neovascular age-related macular degeneration; Expert Opin. Investig. Drugs 18 637 5 Comandone et al. (2021) Antiangiogenic Therapy in Clear Cell Renal Carcinoma (CCRC): Pharmacological Basis and Clinical Results; Cancers (Basel) 13 5896
-20°C
TARGET: Kinase -- DISEASE AREA: Cancer; Inflammation