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Cabozantinib研究進(jìn)展

發(fā)布日期:2017-11-01   瀏覽次數(shù):0
核心提示:a href=https://www.medchemexpress.com/Cabozantinib.htmlCabozantinib/a產(chǎn)品描述:Cabozantinib is a potent multiple RTKs in
Cabozantinib產(chǎn)品描述:Cabozantinib is a potent multiple RTKs inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50 of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.IC50 & Target: IC50: 0.035 nM (VEGFR2), 1.3 nM (c-Met), 4.6 nM (Kit), 7 nM (Axl), 11.3 nM (Flt3)[1]In Vitro: Cabozantinib is a potent inhibitor of MET and VEGFR2 with IC50 values of 1.3 and 0.035 nM, respectively. MET-activating kinase domain mutations Y1248H, D1246N, or K1262R are also inhibited by Cabozantinib (IC50=3.8, 11.8, and 14.6 nM, respectively). Cabozantinib displays strong inhibition of several kinases that have also been implicated in tumor pathobiology, including KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). In cellular assays, Cabozantinib inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42


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