SU5408 is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.

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)[1].

[1]. Sun L, et al. Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity towardparticular receptor tyrosine kinases. J Med Chem. 1998 Jul 2;41(14):2588-603.