2. Protein Tyrosine Kinase/RTK Apoptosis
  3. c-Met/HGFR Apoptosis
  4. Capmatinib

Capmatinib  (Synonyms: INC280; INCB28060)

Cat. No.: HY-13404 Purity: 99.92%
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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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Capmatinib Chemical Structure

Capmatinib Chemical Structure

CAS No. : 1029712-80-8

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Based on 11 publication(s) in Google Scholar

Other Forms of Capmatinib:

Capmatinib Related Antibodies

Top Publications Citing Use of Products

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

    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

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    Description

    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[1][2][3].

    IC50 & Target

    IC50: 0.13 nM (c-MET)[1]
    In Vitro

    Capmatinib (INCB28060) inhibits c-MET phosphorylation with an IC50 value of approximately 1 nM and a concentration of approximately 4 nM inhibits c-MET more than 90%, which is? reversible and the effect is significantly reduced in several hours after the compound is removed and completely disappeared by 48 hours[1].
    ? Capmatinib (INCB28060) (0-10000 nM; 72 h) inhibits the proliferation of SNU-5, S114, H441 and U-87MG[1].
    ? Capmatinib (INCB28060) (0.06-62.25 nM; 2h) effectively inhibits phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5[1].
    ? Capmatinib (INCB28060) (0.24-63 nM; over night) prevents HGF-stimulated H441 cell migration[1].
    ? Capmatinib (INCB28060) (0.5-50 nM; 20 min) suppresses phosphorylation of both EGFR and HER-3 rapidly[1].
    ? Capmatinib (INCB28060) (0-333 nM; 24 h) induces apoptosis in SNU-5 cells[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Capmatinib Related Antibodies

    Cell Viability Assay[1]

    Cell Line: SNU-5, S114, H441 and U-87MG
    Concentration: 0-10000 nM
    Incubation Time: 72 h
    Result: Inhibited the cell viability of SNU-5 and S114, as well as the colony formation of H441 and U-87MG, with IC50 values of 1.2 nM, 12.4 nM, ~0.5 nM and 2 nM, respectively.

    Cell Migration Assay [1]

    Cell Line: H441 (stimulated with 50 ng/mL recombinant human HGF for 24h)
    Concentration: 0.24, 1, 4, 16 and 63 nM
    Incubation Time: Over night
    Result: Prevented HGF-stimulated H441 cell migration, with IC50 of approximately 2 nM, and less cell migration at 16 nM.

    Western Blot Analysis[1]

    Cell Line: SNU-5
    Concentration: 0.06, 0.24, 0.98, 3.91, 15.63 and 62.25 nM
    Incubation Time: 2 h
    Result: Effectively inhibited phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5.

    Western Blot Analysis[1]

    Cell Line: H1993 cells
    Concentration: 0.5, 5 and 50 nM
    Incubation Time: 20 min
    Result: Suppressed phosphorylation of both EGFR and HER-3 rapidly and as effectively as the compound inhibited c-MET phosphorylation in H1993 cells.

    Apoptosis Analysis[1]

    Cell Line: SNU-5 cells
    Concentration: 0.017, 0.15, 1.37, 12.33, 111 and 333 nM
    Incubation Time: 24 h
    Result: Effectively induced DNA fragmentation.
    In Vivo

    Capmatinib (INCB28060) (1-30 mg/kg; PO, twice daily, for 2 weeks) exhibits dose-dependent inhibition of tumor growth, and shows well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss in U-87MG tumor mice model[1].
    ? Capmatinib (INCB28060) (0.03-10 mg/kg; PO, single dosage) causes inhibition of c-MET phosphorylation in S114 tumor mice model[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female Balb/c nu/nu mice (inoculated subcutaneously with 5×106 U-87MG glioblastoma cells)[1]
    Dosage: 1, 3, 10 and 30 mg/kg
    Administration: PO, twice daily, for 2 weeks
    Result: Exhibited dose-dependent inhibition of tumor growth with 35% and 76% at 1 and 3 mg/kg once daily; resulted in partial regressions in 6 of 10 U-87MG tumor-bearing mice at 10 mg/kg once daily; and showed well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss.
    Animal Model: Female Balb/c nu/nu mice (inoculated subcutaneously with 4×106 S114 tumor cells)[1]
    Dosage: 0.03, 0.1, 0.3, 1, 3 and 10 mg/kg
    Administration: PO, single dosage
    Result: Caused approximately 50% and 90% inhibition of c-MET phosphorylation at 0.03 and 0.3 mg/kg after administration of 30 min, and inhibition of phospho-c-MET exceeded 90% after 7 hours.
    Clinical Trial
    Molecular Weight

    412.42

    Formula

    C23H17FN6O
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(NC)C1=CC=C(C2=NN3C(N=C2)=NC=C3CC4=CC=C5N=CC=CC5=C4)C=C1F
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 5 mg/mL (12.12 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 4 mg/mL (9.70 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4247 mL 12.1236 mL 24.2471 mL
    5 mM 0.4849 mL 2.4247 mL 4.8494 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Purity & Documentation

    Purity: 99.92%

    COA (252 KB) LCMS (112 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.4247 mL 12.1236 mL 24.2471 mL 60.6178 mL
    5 mM 0.4849 mL 2.4247 mL 4.8494 mL 12.1236 mL
    DMSO 10 mM 0.2425 mL 1.2124 mL 2.4247 mL 6.0618 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Capmatinib Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Capmatinib1029712-80-8INC280 INCB28060INC 280INC-280INCB28060INCB 28060INCB-28060c-Met/HGFRApoptosisorally activeATP competitiveSNU-5S114H441U-87MGBalb/c nu/nu miceInhibitorinhibitorinhibit

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