Potent ATP-competitive PDGFR and VEGFR inhibitor (Ki
= 5 and 6 nM, respectively); inhibits phosphorylation of c-Kit and suppresses the growth of mast cell lines expressing mutant Kit, inducing cell cycle arrest and apoptosis. Also inhibits FGFR1 (Ki
= 0.5 μ
M). Effective in vivo
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Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors.
Liao et al.