产品描述:
NVP-ACC789 is an inhibitor of VEGF receptor tyrosine kinases (VEGFRs; IC50s = 0.38, 0.02, 0.18, and 0.23 μM for human VEGFR1, 2, 3, and mouse Vegfr2, respectively).{37221} It is selective for VEGFRs over FGFRs and PDGFRα (IC50s = >10 μM) but has activity at PDGFRβ (IC50 = 1.4 μM) in an enzyme assay. NVP-ACC789 inhibits VEGF-induced VEGFR2 autophosphorylation (IC50 = 11.5 nM in CHO cells transfected with the human receptor). It also inhibits VEGF- and bFGF-induced angiogenesis and cell migration of BAE and BME cells. In vivo, NVP-ACC789 blocks bFGF- and VEGF-induced angiogenesis (ED50s = 9 and 26 mg/kg, respectively) in a mouse model of growth factor-induced angiogenesis.