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首页> 产品展示> Tivozanib (AV-951)

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Tivozanib (AV-951)

品牌 厂商性质 产地 货期
阿拉丁 生产商 上海 现货

在线咨询 询底价
产品参数
货号 CAS号 操作
T126012-25mg 475108-18-0 询底价
T126012-5mg 475108-18-0 询底价
T126012-100mg 475108-18-0 询底价
产品介绍

  • 分子式 C22H19ClN4O5
  • 分子量454.87

属性

溶解性 DMSO ≥36mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
存贮条件 储存温度-20°C

描述

产品介绍 Tivozanib (AV-951)是VEGFR抑制剂,对VEGFR1,2和3的IC50分别为30 nM,6.5 nM和15 nM,还能抑制PDGFR和c-Kit,对FGFR-1,Flt3,c-Met,EGFR和IGF-1R的抑制性较低。
备注 Tivozanib (AV-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 0.21 nM/0.16 nM/0.24 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met EGFR and IGF-1R. Phase 3.
生化机理 AV-951 is a novel quinoline-urea derivative. AV-951 blocks VEGF-dependent activation of mitogen-activated protein kinases and proliferation of endothelial cells [1]. 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.
别名 AV-951;AV951;AV 951;N-[2-氯-4-[(6,7-二甲氧基-4-喹啉基)氧基]苯基]-N'-(5-甲基-3-异恶唑基)脲;AV-951;AV951;AV 951;N-[2-Chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl]-N'-(5-methyl-3-isoxazolyl)urea

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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途