Sunitinib, Malate Salt (Sunitinib Maleate, Sutent, SU-11248, PHA-290940AD, PNU-290940AD, CAS 341031-54-7), >99%

LC Laboratories' Product Number S-8803 - Sunitinib, Malate Salt (Sunitinib Maleate, Sutent, SU-11248, PHA-290940AD, PNU-290940AD), >99% - for research use only. Sunitinib and its active metabolite (SU012662) are selective inhibitors of multiple receptor tyrosine kinases, including platelet-derived growth factor receptor and vascular endothelial growth factor receptor, that are associated with tumor growth and angiogenesis. Sunitinib is a potent inhibitor of colony-stimulating factor-1 receptor kinase in an enzyme assay, with an IC50 value of 7 nM, and inhibits receptor phosphorylation in a cellular assay with an IC50 value of 61 nM. Sunitinib dose-dependently inhibited stem cell factor (SCF)-induced phosphotyrosine levels on KIT (IC50 = 1 - 10 nM) and reduced SCF-stimulated ERK1/2 phosphorylation with an IC50 value consistent with that for inhibition of KIT phosphotyrosine levels. Sunitinib also inhibited SCF-stimulated proliferation in NCI-H526 cells (IC50 = 2 nM). Sunitinib dose-dependently inhibited FLT3-ITD phosphorylation (IC50 = 50 nM) following a 2-hour treatment. For the FLT3-ITD cell line MV-4-11, which expresses FLT3-ITD mutant, sunitinib dramatically inhibited cellular proliferation with an IC50 of 1 to 10 nM. Sunitinib is the active ingredient in the drug sold under the trade name Sutent. This drug is a small molecule receptor tyrosine kinase inhibitor that has been approved in at least one country for the treatment of patients having gastrointestinal stromal tumors (GIST) or renal cell carcinoma (RCC).

• Supplier: LC Laboratories
• Product #: S-8803
• Sku #: S-8803_10g