现货,Tivozanib (AV-951),CAS号:475108-18-0,美国进口,受体酪氨酸激酶(RTK) ,VEGFR , VEGFR 抑制剂和化合物,selleck,S1207

信号转导通路: 受体酪氨酸激酶(RTK) >> VEGFR >> VEGFR 抑制剂 >> Tivozanib (AV-951)http://www.selleck.cn/av-951-S1207.html

技术数据:

分子量(MW): 454.86

化学式:

C22H19ClN4O5

 

溶解度: DMSO ≥39mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 475108-18-0

生物活性

 

 

Tivozanib (AV-951) is an orally bioavailable potent VEGFR-1, 2 and 3, cKit and PDGFR inhibitor with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM, respectively. Tivozanib (AV-951) has potential antiangiogenic and antineoplastic activities. Tivozanib (AV-951) inhibits c-Kit and PDGFR at 10-times higher concentrations. Tivozanib (AV-951) is a novel oral quinoline urea derivative. Preclinical data indicate that AV-951 blocks the proliferation and migration of endothelial cells in vitro, and suppresses angiogenesis and growth of human tumor xenografts in vivo. Tivozanib has been shown to be safe and orally bioavailable when given to cancer patients. Tivozanib (AV-951) is under early clinical investigation for the treatment of renal cell carcinoma and non-small cell lung carcinoma, as well as in combination with other chemotherapies in breast, colorectal, and other gastrointestinal cancer patients. [1]

 

 

 

参考文献

Drugs of the Future Campas, C. et al Drugs Fut 2009;34(10): 793

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