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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL|
The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis.
Martiny-Baron G, et al. Angiogenesis. 2010 Sep;13(3):259-67. PMID: 20803239.
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