NVP-BHG712 is a small molecule specific EphB4, VEGFR2, c-raf, c-src and c-Abl kinase inhibitor with ED50 of 25 nM, 4.2, 0.4, 1.3 and 1.7¦ÌM, respectively. NVP-BHG712 inhibits multiple Eph receptor kinases. NVP-BHG712 inhibits VEGF driven angiogenesis. In a panel of more than 40 in vitro kinase assays, NVP-BHG712 showed excellent selectivity. Only c-raf, c-src and c-abl showed moderate inhibition as judged from our biochemical assays. In cell based assays ED50 for inhibition of EphB4 autophosphorylation was found to be 25 nM and thereby be roughly 200 fold more potent on EphB4 than on VEGFR2. NVP-BHG712 inhibited dose dependently VEGF stimulated tissue formation and vascularization in this model. Already at doses of daily 3 mg/kg p.o administration we observed significant inhibition, and daily administration of 10 mg/kg/kg p.o. was sufficient to reverse VEGF enhanced tissue formation and vessel growth

June 21, 2017

prudect name : NVP-BHG712 is a small molecule specific EphB4, VEGFR2, c-raf, c-src and c-Abl kinase inhibitor with ED50 of 25 nM, 4.2, 0.4, 1.3 and 1.7¦ÌM, respectively.
NVP-BHG712 inhibits multiple Eph receptor kinases. NVP-BHG712 inhibits VEGF driven angiogenesis. In a panel of more than 40 in vitro kinase assays, NVP-BHG712 showed excellent selectivity. Only c-raf, c-src and c-abl showed moderate inhibition as judged from our biochemical assays. In cell based assays ED50 for inhibition of EphB4 autophosphorylation was found to be 25 nM and thereby be roughly 200
fold more potent on EphB4 than on VEGFR2. NVP-BHG712 inhibited dose dependently VEGF stimulated tissue formation and vascularization in this model. Already at doses of daily 3 mg/kg p.o administration we observed significant inhibition, and daily administration of 10 mg/kg/kg p.o. was sufficient to
reverse VEGF enhanced tissue formation and vessel growth
NVP-BHG712

Synonyms: CAS NO: 940310-85-0Molecular Formula: C26H20F3N7OMolecular Weight: 503.48Purity: 98% minSolubility: In DMSOStorage: −20°C


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References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18536095