Sunitinib Malate VEGFR Inhibitors

Sunitinib, also known as SU11248, is the orally bioavailable malate salt of an indolinone-based tyrosine kinase inhibitor with potential antineoplastic activity. Sunitinib was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 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.

Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.

Related Prodcuts:

Sorafenib; Cabozantinib; Cabozantinib malate; Ponatinib; Axitinib; Vandetanib; Nintedanib; Regorafenib; Pazopanib HCl; Pazopanib; Cediranib; Dovitinib; Lenvatinib; Tivozanib; Sorafenib Tosylate; Sunitinib

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