| A multi-kinase inhibitor targeting several receptor tyrosine kinases (RTK). 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 dose-dependently inhibited stem cell factor (SCF)-induced phosphotyrosine levels on KIT (IC50 = 1-10nM) 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 = 2nM). Synonyms: Sutent, N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, (2S)-hydroxy-butanedioic acid, Sunitinib Malate, SU-11248, PHA-290940AD, PNU-290940AD CAS No: 341031-54-7 Molecular Formula: C26H33FN4O7 Molecular Weight: 532.56 Appearance: Yellow to orange powder Purity: 98% Melting Point: 187-198C Solubility: Soluble in DMSO. Poorly soluble in dH2O and ethanol. DMF: 1mg/ml, DMSO: 5mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25mg/ml Storage and Stability: May be stored at RT for short-term only. Long-term storage is recommended at -20C. For maximum recovery of product, centrifuge the original vial prior to removing the cap. |
