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产品介绍
产品介绍
产品信息
抗原名称
VEGFR2,Flk1,FGFR1,VEGFR1
商品描述
Brivanib (BMS-540215)是一种ATP竞争性的VEGFR2抑制剂，IC50为25 nM，对VEGFR-1和FGFR-1抑制作用适中，但比作用于PDGFR-β效果强240多倍。Brivanib也抑制VEGFR-1和FGFR-1，IC50分别为0.38和0.148 μM。Brivanib对PDGFR-β, EGFR, LCK, PKCα 或JAK-3作用效果不大，IC50 都大于1900 nM。Brivanib 可抑制VEGF刺激的HUVECs细胞增殖，IC50为40 nM,作用于FGF刺激的HUVECs细胞增殖，IC50为276 nM。
分子量
370.38
纯度
>98%
可溶性
DMSO
In vitro(体外研究)
Brivanib also inhibits VEGFR1 and FGFR-1 with IC50 of 0.38 μM and 0.148 μM. Brivanib is not sensitive to PDGFRβ, EGFR, LCK, PKCα or JAK-3 with IC50 all above 1900 nM. Brivanib could inhibit the proliferation of VEGF-stimulated HUVECs with IC50 of 40 nM, compared to 276 nM in FGF-stimulated HUVECs. On the other hand, Brivanib exhibits low activity to tumor cell lines.
In vivo(体内研究)
Brivanib displays antitumor activities in H3396 xenograft in athymic mice. At a dose of 60 and 90 mg/kg (p.o.), Brivanib completely inhibits the tumor growth, with TGI of 85% and 97%, respectively. Moreover, Brivanib significantly suppresses tumor growth in Hepatocellular carcinoma (HCC) xenografts, which due to the decrease in phosphorylation of VEGFR2. The results show that the tumor weights in 06-0606 xenograft mice are 55% and 13%, compared with the controls at a dose of 50 mg/kg and 100 mg/kg. Brivanib is suggested to be efficient in treatment of HCC.
背景
别名
BMS-540215；布立尼布
分子式
C19H19FN4O3
CAS号
649735-46-6
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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