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NVP-BHG712
点击次数：287发布时间：2013/4/1 10:29:17
更新日期：2022/8/19 17:45:40
所 在 地：美洲
产品型号：
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详细内容
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]
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]
