Sunitinib free base (SU-11248)

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.

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