NVP-BHG712 (C09-0990-507)

InformationNVP-BHG712 is a specificEphB4inhibitor withED50of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl withIC50of 0.395 μM, 1.266 μM and 1.667 μM, respectively.In vitroNVP-BHG712 treatment also dose dependently leads to the inhibition of RTK autophosphorylation in stable transfected A375 melanoma cells with EC50 of 25 nM and 4.2 μM for EphB4 and VEGFR2, respectively.In vivoIn a growth factor-induced angiogenesis model, NVP-BHG712 (3 mg/kg, p.o) significantly suppresses VEGF stimulated tissue formation and vascularization by inhibiting EphB4 forward signaling. Furthermore, NVP-BHG712 (10 mg/kg/kg, p.o.) potently reverses VEGF enhanced tissue formation and vessel growth. NVP-BHG712 (3 mg/kg, p.o.) shows a long lasting exposure with concentrations around 10 μM in plasma as well as in lung and liver tissue for up to 8 hours, and thus results in a long lasting inhibition of EphB4 kinase activity in mice.Cell Datacell lines：WST-1, ANBL-6 cellsConcentrations：Incubation Time：Powder Purity:≥97%. Specification: 10mM in DMSO Molecular Formula: C26H20F3N7O Molecular Weight: 503.48