NVP-BHG712

NVP-BHG712 is a specific small molecular, selective inhibitor of EphB4 kinase which inhibits EphB4 and VEGFR2 with ED50 of 25 nM and 4.2 μM, respectively. NVP-BHG712 is also an inhibitor of c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM. NVP-BHG712 inhibits EphB4 autophosphorylation in transiently transfected HEK 293 cells. NVP-BHG712 blocks Ephrin receptor autophosphorylation and VEGF-induced angiogenesis in vivo. NVP-BHG712 inhibits VEGF driven vessel formation, while it has only little effects on VEGF receptor (VEGFR) activity in vitro or in cellular assays. Furthermore, NVP-BHG712 shows excellent pharmacokinetic properties and potently inhibits EphB4 autophosphorylation in tissues after oral administration.