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产品介绍
产品介绍
产品信息
抗原名称
VEGFR2 ,VEGFR3 ,EphB2 ,VEGFR1 ,PDGFRα
商品描述
Tivozanib (AV-951)是一种有效的，选择性VEGFR抑制剂，作用于VEGFR1/2/3时，IC50分别为0.21 nM/0.16 nM/0.24 nM，也抑制PDGFR和c-Kit，作用于FGFR-1， Flt3， c-Met EGFR和IGF-1R活性较弱。AV-951 也抑制PDGFRß和c-Kit的磷酸化作用，IC50 分别为1.72nm 和1.63nM。AV-951阻断VEGF依赖的MAPK活性和内皮细胞增殖。AV-951是新型喹啉-尿素派生物。
分子量
454.86
纯度
98%
可溶性
DMSO ：16 mg/mL (35.2 mM)
In vitro(体外研究)
AV-951 is a novel quinoline-urea derivative. AV-951 blocks VEGF-dependent activation of mitogen-activated protein kinases and proliferation of endothelial cells.
In vivo(体内研究)
In vivo studies show that AV-951 also decreases the micro vessel density and suppresses VEGFR2 phosphorylation levels in tumor xenografts, especially at a concentration of 1mg/kg (p.o. administration). AV-951 shows almost complete inhibition of tumor xenografts growth (TGI>85%) in athymic rats. Another study in rat peritoneal disseminated tumor model shows that AV-951 could prolong the survival of the tumor-bearing rats with the MST of 53.5 days. AV-951 displays antitumor activity against many human tumor xenografts including lung, breast, colon, ovarian, pancreas and prostate cancer.
背景
别名
替沃扎尼；AV-951；KRN951
分子式
C22H19ClN4O5
CAS号
475108-18-0
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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