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Glumetinib

CAS No. 1642581-63-2

Glumetinib ( SCC244 | SCC 244 )

产品货号. M12497 CAS No. 1642581-63-2

Glumetinib (SCC 244) 是一种新型有效且高选择性的 c-Met 激酶抑制剂,IC50 为 0.42 nM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥915 有现货
10MG ¥1401 有现货
25MG ¥2365 有现货
50MG ¥3540 有现货
100MG ¥5233 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    Glumetinib
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    Glumetinib (SCC 244) 是一种新型有效且高选择性的 c-Met 激酶抑制剂,IC50 为 0.42 nM。
  • 产品描述
    Glumetinib (SCC 244)?is a novel potent and highly selective inhibitor of c-Met kinase with IC50 of 0.42 nM; displays high selectivity versus 312 other tested protein kinases; profoundly and specifically inhibits c-Met signal transduction and suppresses the c-Met-dependent neoplastic phenotype of tumor and endothelial cells; exhibits robust in vivo antitumor activity in NSCLC and hepatocellular carcinoma models.Lung Cancer Preclinical(In Vitro):Glumetinib (SCC244) (0-10 nM; 72 hours) elicits selective and profound effects against c-Met–driven cancer cell proliferation.Glumetinib (0-50 nM; 24 hours) induces G1–S phase cell-cycle arrest in c-Met–addicted human cancer cells.(In Vivo):Glumetinib (2.5-10 mg/kg; p.o.; once daily for 2-3 weeks) significantly inhibits c-Met–driven tumor growth in cancer CDX models.Glumetinib shows significant antitumor efficiency in NSCLC and HCC tumor PDX models with MET aberration.
  • 体外实验
    Glumetinib (SCC244) (0-10 nM; 72 hours) elicits selective and profound effects against c-Met–driven cancer cell proliferation.Glumetinib (0-50 nM; 24 hours) induces G1–S phase cell-cycle arrest in c-Met–addicted human cancer cells. Cell Proliferation Assay Cell Line:EBC-1, SNU-5, MKN-45, BaF3/TPR-Met cells Concentration:0-10 nM Incubation Time:72 hours Result:Specifically and potently inhibited proliferation of c-Met–addicted human cancer cells (IC50 ranging 0.5 to 2.45 nM for EBC-1, SNU-5, MKN-45, BaF3/TPR-Met cells ).Cell Cycle AnalysisCell Line:EBC-1 and MKN-45 cells Concentration:0-50 nM Incubation Time:24 hours Result:Consistently induced G1–S cell-cycle arrest.
  • 体内实验
    Glumetinib (2.5-10 mg/kg; p.o.; once daily for 2-3 weeks) significantly inhibits c-Met–driven tumor growth in cancer CDX models.Glumetinib shows significant antitumor efficiency in NSCLC and HCC tumor PDX models with MET aberration. Animal Model:Female nude mice (4-6 weeks old) (MKN-45 model) Dosage:10, 5, 2.5 mg/kg Administration:P.o.; once daily for 2-3 weeks Result:Significantly inhibited tumor growth with inhibitory rates of 99.3%, 88.6%, and 63.6% at doses of 10, 5, and 2.5 mg/kg, respectively.
  • 同义词
    SCC244 | SCC 244
  • 通路
    Angiogenesis
  • 靶点
    c-Met/HGFR
  • 受体
    c-Met
  • 研究领域
    Cancer
  • 适应症
    Lung Cancer

化学信息

  • CAS Number
    1642581-63-2
  • 分子量
    459.488
  • 分子式
    C21H17N9O2S
  • 纯度
    >98% (HPLC)
  • 溶解度
    10 mM in DMSO
  • SMILES
    O=S(N1N=CC2=NC=C(C3=CN(C)N=C3)C=C21)(C4=CN=C5C=CC(C6=CN(C)N=C6)=CN54)=O
  • 化学全称
    6-(1-Methyl-1H-pyrazol-4-yl)-1-[[6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]sulfonyl]-1H-pyrazolo[4,3-b]pyridine

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Ai J, et al. Mol Cancer Ther. 2017 Dec 13. pii: molcanther.0368.2017.
产品手册
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