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SKLB1002研究進展

發(fā)布日期：2017-11-02   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/SKLB1002.htmlSKLB1002/a產(chǎn)品描述：SKLB1002 is a novel and potent VEGFR-2 inhibitor
SKLB1002產(chǎn)品描述：SKLB1002 is a novel and potent VEGFR-2 inhibitor with an IC50 value of 32 nM.IC50 Value: 32 nM [1]Target: VEGFR-2in vitro: SKLB1002 showed potent inhibition of VEGFR2 kinase activity (IC50 = 32 nmol/L), which was similar with the positive drugs vandetanib (IC50 = 40 nmol/L) and sunitinib (IC50 = 9 nmol/L). SKLB1002 significantly inhibited endothelial cell proliferation with an IC50 value of 11.9 μmol/L. However, vandetanib and sunitinib inhibited cell viability at a much lower concentration with an IC50 value of 3.8 μmol/L and 1.9 μmol/L, respectively [1].in vivo: In vivo zebrafish model experiments showed that SKLB1002 remarkably blocked the formation of intersegmental vessels in zebrafish embryos. It was further found to inhibit a new microvasculature in zebrafish embryos induced by inoculated tumor cells. Finally, compared with the solvent control, administration of 100 mg/kg/d SKLB1002 reached more than 60% inhibition against human tumor xenografts in athymic mice [1]. Sys


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