溶解性 | DMSO ≥36mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
存贮条件 | 储存温度-20°C |
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 |
Tivozanib (AV-951),抑制剂
Tivozanib (AV-951) (订货以英文为准)
编号:T126012
CAS号:475108-18-0
分子式:C22H19CLN4O5
分子量:454.86
产品名称 | Tivozanib (AV-951) |
中文名称 | Tivozanib (AV-951),抑制剂 |
CAS号 | 475108-18-0 |
MDL编码 | MFCD15146788 |
分子式(M.F.) | C22H19CLN4O5 |
分子量(M.W.) | 454.86 |
储存条件 | -20°C储存 |
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