Sunitinib Malate (Sutent)

1 g. Purity >99%. CAS# 341031-54-7. 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. Soluble in DMSO (40 mg/ml). Store cool and dry at -20C. Protect from light.