NVP-BHG712CAS号： 940310-85-0分子式： C26H20F3N7O分子量： 503.48描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 | |
| 描述 |
NVP-BHG712是一种特异性的EphB4抑制剂，ED50为25 nM，区别于对VEGFR和EphB4的抑制，对c-Raf， c-Src和c-Abl也具有抑制活性，IC50分别为0.395 μM， 1.266 μM和1.667 μM。NVP-BHG712作用于稳定转染的A375黑色素瘤细胞，也抑制RTK自磷酸化，这种作用存在剂量依赖性，作用于EphB4和VEGFR2时, EC50分别为25 nM和 4.2 μM。 |
| 纯度 |
>98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
NVP-BHG712
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| 可溶性/溶解性 |
10 mM in DMSO
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| 生物活性 | |
| 靶点 |
EphB4 ,C-Raf ,c-Src ,c-Abl
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| In vitro(体外研究) |
NVP-BHG712 treatment also dose dependently leads to the inhibition of RTK autophosphorylation in stable transfected A375 melanoma cells with EC50 of 25 nM and 4.2 μM for EphB4 and VEGFR2, respectively.
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| In vivo(体内研究) |
In a growth factor-induced angiogenesis model, NVP-BHG712 (3 mg/kg, p.o) significantly suppresses VEGF stimulated tissue formation and vascularization by inhibiting EphB4 forward signaling. Furthermore, NVP-BHG712 (10 mg/kg/kg, p.o.) potently reverses VEGF enhanced tissue formation and vessel growth. NVP-BHG712 (3 mg/kg, p.o.) shows a long lasting exposure with concentrations around 10 μM in plasma as well as in lung and liver tissue for up to 8 hours, and thus results in a long lasting inhibition of EphB4 kinase activity in mice.
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| 参考文献 | |
| 参考文献 |
The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis.
Martiny-Baron G,et al. Angiogenesis. 2010 Sep;13(3):259-67. PMID: 分子结构图
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