产品
编 号：F104042
分子式：C22H22N4O4S
分子量：438.5
分子式：C22H22N4O4S
分子量：438.5
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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2mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1265965-22-7
产品详情
生物活性：
S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
体内研究：
In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 is established and correlated well with impact on tumor growth. MET, AXL, and the FGFRs have all been implicated in resistance to VEGF/VEGFR inhibitors such as bevacizumab. Combination of S49076 with bevacizumab in colon carcinoma xenograft models leads to near total inhibition of tumor growth. S49076 alone caused tumor growth arrest in bevacizumab-resistant tumors.
体外研究：
S49076 potently blocks cellular phosphorylation of MET, AXL, and FGFRs and inhibits downstream signaling. S49076 inhibits the proliferation of MET- and FGFR2-dependent gastric cancer cells, blocks MET-driven migration of lung carcinoma cells, and inhibits colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. Total inhibition of MET phosphorylation is seen after 2 hours of incubation with 10 nM S49076 and an with an IC50 of 2 nM. S49076 inhibits MET phosphorylation on this site in GTL-16 gastric carcinoma cells with an IC50value of 3 nM. The IC50for AXL inhibition by S49076 is 56 nM. S49076 inhibits AXL signaling via AKT with an IC50of 33 nM.
S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
体内研究：
In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 is established and correlated well with impact on tumor growth. MET, AXL, and the FGFRs have all been implicated in resistance to VEGF/VEGFR inhibitors such as bevacizumab. Combination of S49076 with bevacizumab in colon carcinoma xenograft models leads to near total inhibition of tumor growth. S49076 alone caused tumor growth arrest in bevacizumab-resistant tumors.
体外研究：
S49076 potently blocks cellular phosphorylation of MET, AXL, and FGFRs and inhibits downstream signaling. S49076 inhibits the proliferation of MET- and FGFR2-dependent gastric cancer cells, blocks MET-driven migration of lung carcinoma cells, and inhibits colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. Total inhibition of MET phosphorylation is seen after 2 hours of incubation with 10 nM S49076 and an with an IC50 of 2 nM. S49076 inhibits MET phosphorylation on this site in GTL-16 gastric carcinoma cells with an IC50value of 3 nM. The IC50for AXL inhibition by S49076 is 56 nM. S49076 inhibits AXL signaling via AKT with an IC50of 33 nM.
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