化学名称 : PD173074/PD-173074/
CAS : 219580-11-7
英文同义词: N-[2-[[4-(Diethylamino)butyl]amino] -6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-y l]-N'-(1,1-dimethylethyl)urea
储存条件:at -20℃ 2 years
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 1.7μM, 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.