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Capmatinib

(別名: INC280; INCB28060)
27 Cited Publications
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Based on 27 publication(s) in Google Scholar

Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase.

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  • 純度: 99.71%
  • CAS 番号: 1029712-80-8
  • 分子式: C23H17FN6O
  • 分子量:412.42
  • 保管条件:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 2 years , -20°C, 1 year
  • Capmatinib Chemical Structure
    Capmatinib 構造式
  • Experimental Validation Results for Capmatinib
  • Experimental Validation Results for Capmatinib
  • Experimental Validation Results for Capmatinib
  • Experimental Validation Results for Capmatinib
  • Experimental Validation Results for Capmatinib
  • Experimental Validation Results for Capmatinib
CAS 番号: 1029712-80-8
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  • In Vivo Efficacy Study
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  • Cell Proliferation/Viability Assay
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  • Capmatinib Chemical Structure
    Capmatinib Chemical Structure
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    Capmatinib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 17:e00806. [Abstract]

    Customer Validation
     A) Orthotopic inoculated KPC tumors from the control, Capmatinib (INC280) monotherapy, DTA-1 monotherapy and combined therapy groups. B) Quantification of tumor weights under different treatment.Male C57BL/6 mice (KPC cells，orthotopic pancreatic tumor model ), 1) vehicle (5% DMSO + 45% PEG300/5% Tween80 + 50% ddH2O) + IgG control, 2) MET inhibitor monotherapy: INC280 (10 mg kg day−1 for 8 days) + IgG, 3) GITR agonist monotherapy: DTA‐1 (100 µg mouse day−1 for 4 days) + vehicle, and 4) combination therapy: INC280+ DTA‐1. INC280 was formulated in a vehicle solution of DMSO/PEG300/Tween80/ddH₂O (5:45:5:50, v/v) and administered by intraperitoneal injection.

  • 1/16

    Capmatinib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 17:e00806. [Abstract]

    Customer Validation
     Flowcytometry analysis of GzmB , and TNF-α expression in CD8+ T cells under different treatment. Male C57BL/6 mice (KPC cells，orthotopic pancreatic tumor model ), 1) vehicle (5% DMSO + 45% PEG300/5% Tween80 + 50% ddH2O) + IgG control, 2) MET inhibitor monotherapy: INC280 (Capmatinib, 10 mg kg day−1 for 8 days) + IgG, 3) GITR agonist monotherapy: DTA‐1 (100 µg mouse day−1 for 4 days) + vehicle, and 4) combination therapy: INC280+ DTA‐1. INC280 was formulated in a vehicle solution of DMSO/PEG300/Tween80/ddH2O (5:45:5:50, v/v) and administered by intraperitoneal injection.

  • 1/16

    Capmatinib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Feb 19;26(4):1766. [Abstract]

    Customer Validation
     In the 3D culture system, MPE primary cells formed stable spheroids within 96 h. Drug sensitivity assays using the 3D tumorsphere model showed that Giotrif (afatinib) at 60 nM and Capmatinib (0.8 nM; 96 h) at 6.5 nM achieved IC50.

  • 1/16

    Capmatinib purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2025 Feb;19(2):474-495. [Abstract]

    Customer Validation
     Capmatinib (0.5,1 μM; 24 h) toxicity was also tested through MTT tests at higher concentration.

  • 1/16

    Capmatinib purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2025 Feb;19(2):474-495. [Abstract]

    Customer Validation
     (A)Graphical representation of tumour volume over time after subcutaneous injection of PC3M Ctrl, PC3M ETV1 and PC3M ERG cells. The tumour volume of the mice was monitored by palpation. (B) Graphical representation of the final tumour volume of mice having been treated or not with Capmatinib.8‐week‐old male NSG‐hHGFki mice (PC3M cells), Capmatinib (10 mg/kg; oral gavage 5 days a week, 30 days).

  • 1/16

    Capmatinib purchased from MedChemExpress. Usage Cited in: Wayne State University. 2014 Jan.

    Customer Validation
     The c-Met Inhibitor INC280 Reveals HGF Activation of c-Met Leads to β4 Activation. (A) Dose-dependent assay to determine the concentration of INC280 required to prevent HGF-induced c-Met phosphorylation. Cells are pre-treated for two hours with INC280 at the indicated concentrations and then stimulated with 50 ng/mL HGF for 30 minutes. Phosphorylated (upper panel) and total c-Met (lower panel) are analyzed by Western blot. Densitometry represents the ratio of phosphorylated to total c-Met as a p

  • Capmatinib