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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.
| Molecular Weight | 503.48 |
| Formula | C26H20F3N7O |
| CAS Number | 940310-85-0 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related VEGFR/PDGFR Products |
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| (Rac)-SAR131675
(Rac)-SAR131675 is the racemate of SAR131675. |
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