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S81233

LY2801653

源叶(MedMol) 99%
  • 英文名:
  • LY2801653
  • 别名:
  • L1X; N-(3-fluoro-4-((1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide; QCR-139;
  • CAS号:
  • 1206799-15-6
  • 分子式:
  • C30H22F2N6O3
  • 分子量:
  • 552.53
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S81233-5mg 99% ¥500.00元 5 - - - EA 加入购物车
源叶(MedMol) S81233-10mg 99% ¥800.00元 5 - - - EA 加入购物车
源叶(MedMol) S81233-25mg 99% ¥1350.00元 5 - - - EA 加入购物车
源叶(MedMol) S81233-100mg 99% ¥3500.00元 3 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM)
  • 靶点: Ki: 2 nM (c-Met) IC50: 11 nM (MST1R), 7 nM (FLT3), 2 nM (AXL), 10 nM (MERTK), 63 nM (TEK), 0.1/7 nM (DDR1/2), 7 nM (MKNK1/2);DiscoidinDomainReceptor(DDR); FLT; c-Met/HGFR; ROS; ROSKinase
  • 体内研究:
    Merestinib (LY2801653) demonstrates anti-tumor effects in MET amplified (MKN45), MET autocrine (U-87MG, and KP4) and MET over-expressed (H441) xenograft models; and in vivo vessel normalization effects. Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a pharmacodynamic residence time (Koff) of 0.00132 min-1 and t1/2 of 525 min. Merestinib (LY2801653) treatment inhibits MET phosphorylation with a composite TED50 (50 % target inhibition dose) of 1.2 mg/kg and a composite TED90 (90 % target inhibition dose) of 7.4 mg/kg. Merestinib (LY2801653) (20 mg/kg) reduces TFK-1 tumor growth significantly relative to vehicle control. Merestinib (LY2801653) inhibits the growth of intra- and extrahepatic CCC xenograft tumors.
  • 参考文献:
    1. Yan SB, et al. LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models. Invest New Drugs. 2013 Aug;31(4):833-44. 2. Barat S, et al. Targeting c-MET by LY2801653 for treatment of cholangiocarcinoma. Mol Carcinog. 2016 Jan 12.
  • 溶解性: DMSO  :  ≥  32  mg/mL  (57.92  mM)
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.81 ml 9.049 ml 18.099 ml
    5 mM 0.362 ml 1.81 ml 3.62 ml
    10 mM 0.181 ml 0.905 ml 1.81 ml
    50 mM 0.036 ml 0.181 ml 0.362 ml
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