SU5408 is a highly selective, cell-permeable indolin-2-one class of receptor tyrosine kinase (RTK) inhibitor (IC50 = 70 nM) for murine vascular endothelial growth factor receptor 2 (VEGF-R2; KDR/Flk-1). The inhibition is suggested to be competitive with respect to ATP. VEGFR2 Kinase Inhibitor I has been shown to not inhibit PDGF, EGF, and IGF-1 RTK activities (IC50 > 100 μM).
溶解性:DMSO : 6 mg/mL (19.33 mM; Need ultrasonic and warming)
体外研究:
3-Substituted indolin-2-ones have been designed and synthesized as a novel class of tyrosine kinase inhibitors which exhibit selectivity toward different receptor tyrosine kinases (RTKs). These compounds have been evaluated for their relative inhibitory properties against a panel of RTKs in intact cells. SU5408 is found to be the most potent and selective VEGFR2 inhibitor among the compounds. SU5408 shows little or no effect against receptors for platelet-derived growth factor, epidermal growth factor, or insulin-like growth factor (IC50>100 μM).