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Beschreibung

A cell-permeable quinazoline that acts as a potent, ATP-binding site-targeting, VEGFR2-selective inhibitor (IC50 = 32 nM), while exhibiting much reduced potency against c-kit, Ret, FMS, PDGFRalpha, and Aurora A (IC50 = 0.62, 2.5, 2.9, 3.1, and 3.9 µ,M, respectively) and little or no activity against 11 other kinases (IC50 >10 µ,M). An effective antiangiogenesis agent (86%, 92%, and 98% inhibition, respectively, of HUVEC migration, invasion, and tube formation at 10 µ,M, 80% inhibition of zebrafish embryos intersegmental vessel growth at 2.5 µ,M) that significantly suppresses SW620- and HepG2-derived tumor growth in mice (by 72% and 63%, respectively, in 18 days, 100 mg/kg/day, i.p.) in vivo., A cell-permeable quinazoline that acts as a potent, ATP-binding site-targeting, VEGFR2-selective inhibitor (IC50 = 32 nM), while exhibiting much reduced or little activity against 16 other kinases. An effective antiangiogenesis agent (98% inhibition of HUVEC tube formation at 10 µ,M, 80% inhibition of zebrafish embryos intersegmental vessel growth at 2.5 µ,M) that significantly suppresses SW620- and HepG2-derived tumor growth in mice (by 72% and 63%, respectively, in 18 days, 100 mg/kg/day, i.p.) in vivo.