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Beschreibung

A cell-permeable pyridopyrimidine compound that acts as a potent, ATP-competitive, and reversible inhibitor of FGF and VEGF receptors (IC50 = 21.5 nM for FGFR1). It inhibits PDGFR and c-Src only at much higher concentration (IC50 = 17.6 µ,M, 19.8 µ,M, respectively) and exhibits little effect against EGFR, InsR, MEK, and cPKC even at concentrations as high as 50 µ,M. Shown to inhibit the autophosphorylation of endogenous FGFR1 (IC50<5 nM) and overexpressed VEGFR2 (IC50<200 nM) in NIH3T3 cells in vitro, and FGF- and VEGF-induced angiogenesis in mice in vivo.