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Enzymes for Research, Diagnostic and Industrial Use

NVP-BHG712

Cat No.
CEI-0158
Description
NVP-BHG712 can inhibit c-Raf, c-Src and c-Abl with IC50 of 0.395 uM, 1.266 uM and 1.667 uM.
CAS No.
940310-85-0
Molecular Weight
503.48
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
c-Raf, c-Src, c-Abl
Molecular Formula
C26H20F3N7O
Chemical Name
4-methyl-3-(1-methyl-6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide
Solubility
DMSO 101 mg/mL Water
In vitro
As a small molecular weight kinase inhibitor of the EphB4 kinase, NVP-BHG712, which inhibits EphB4 kinase activity in the low nanomolar range in cellular assays. NVP-BHG712 shows excellent pharmacokinetic properties and potently inhibits EphB4 autophosphorylation in tissues after oral administration. 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. NVP-BHG712 can inhibit VEGF induced angiogenesis through inhibiting EphB4, because EphB4 plays an important role in VEGF induced angiogenesis.
In vivo
After oral administration, NVP-BHG712 shows excellent pharmacokinetic properties and potently inhibits EphB4 autophosphorylation in tissues. In vivo, NVP-BHG712 inhibits VEGF driven vessel formation, while it has only little effects on VEGF receptor (VEGFR) activity .
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