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S49076,1265965-22-7

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  • ¥500 - 5800
  • MedChemExpress(MCE)已认证
  • 美国
  • HY-12965
  • 2025年12月05日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 保存条件

      Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

    • 库存

      货期:1-2天

    • 供应商

      MedChemExpress LLC

    • 规格

      10 mM * 1 mL/2 mg/5 mg/10 mg/25 mg/50 mg/100 mg

    规格:10 mM * 1 mL产品价格:¥770.0
    规格:2 mg产品价格:¥500.0
    规格:5 mg产品价格:¥700.0
    规格:10 mg产品价格:¥1100.0
    规格:25 mg产品价格:¥2200.0
    规格:50 mg产品价格:¥3500.0
    规格:100 mg产品价格:¥5800.0

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    S49076

    CAS No. : 1265965-22-7

    MCE 国际站:S49076

    产品活性:S49076是新颖高效的MET, AXL/MERFGFR1/2/3抑制剂, IC50值小于20 nM。

    研究领域:Protein Tyrosine Kinase/RTK

    作用靶点:FGFR  |  c-Met/HGFR

    In Vitro: 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 IC50 value of 3 nM. The IC50 for AXL inhibition by S49076 is 56 nM. S49076 inhibits AXL signaling via AKT with an IC50 of 33 nM.

    In Vivo: 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.

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    图标文献和实验
    相关实验
    • Phosphoamino acid analysis:Mark Kamps's method

      the pH. There have been occasional problems with badly smeared PAAs during electrophoresis at pH 3.5.Something seems to leach out of the wicks and make the PAAs relatively insoluble.Tony thinks it is aluminum.Bart thinks that it's calcium.In any case

    • Phosphoamino acid analysis:Mark Kamps method

      Phosphoamino acid analysis:Mark Kamps's method 1. Label your protein with 32Pi. Then subject the protein to SDS polyacrylamide gel electrophoresis and transfer your gel-fractionated protein to Immobilon-P .  

    • Phosphoamino acid analysis:Mark Kamps method

      Phosphoamino acid analysis:Mark Kamps's method 1. Label your protein with 32Pi. Then subject the protein to SDS polyacrylamide gel electrophoresis and transfer your gel-fractionated protein to Immobilon-P .  

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