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Description: Sunitinib (formerly also known as SU11248; trade name: Sutent) is a potent, orally bioavailable and multi-targeted RTK (receptor tyrosine kinase) inhibitor with potential antitumor activity. It inhibits VEGFR2 (Flk-1) and PDGFRbeta with IC50s of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib was approved by US FDA for the treatment of renal cell carcinoma andimatinib-resistant gastrointestinal stromal tumor in 2006. Sunitinib blocks the tyrosine kinase activities of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor b (PDGFRb), and c-kit, thereby inhibiting angiogenesis and cell proliferation.
References: J Med Chem. 2003 Mar 27; 46(7):1116-9; Clin Cancer Res. 2003 Jan; 9(1):327-37; Blood. 2003 May 1; 101(9):3597-605.
Related CAS: 1221149-36-5 (acetate); 42641-94-5; 1332306-95-2 (oxalate); 1126641-10-8 (maleate); 1275588-72-1 (mesylate); 341031-54-7 (malate); 557795-19-4 (free base); 1327155-72-5 (HCl)
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