NVP-BHG712

NVP-BHG712       
 
        上海义森生物科技有限公司

 

                                                                                                                                                                             

技术数据:

分子量(MW):	503.48
化学式:	C26H20F3N7O
溶解度:	DMSO 101mg/mL   Water <1mg/mL   Ethanol 3mg/mL
纯度:	>99%
稳定性:	at -20℃ 2 years
CAS号:	940310-85-0

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. ^[1]