219580-11-7

PD173074/PD-173074/

219580-11-7

编号ABP000888 化学名称PD173074/PD-173074/ 英文名称 PD173074/PD-173074/ 分子式C28H41N7O3 分子量523.6702 纯度 >97 %

化学名称 : PD173074/PD-173074/

CAS : 219580-11-7

英文名称: PD173074/PD-173074/

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

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

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.

参考文献

[1] Martiny-Baron G et al. Angiogenesis. 2010 Sep;13(3):259-67.

询价