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    Capmatinib (INCB28060; INC-280)
    Capmatinib (INCB28060; INC-280)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0598
    CAS #: 1029712-80-8Purity ≥98%

    Description: Capmatinib (formerly also known as INCB-28060; INC280; Tabrecta) is a novel, potent, orally bioavailable, ATP-competitive inhibitor of c-MET with potential antitumor activity. It inhibits c-MET with an IC50 of 0.13 nM in a cell-free assay, and is inactive against RONβ, as well as EGFR and HER-3. Capmatinib has gained approval for the treatment of adults with metastatic non-small cell lung cancer. c-Met inhibitor INC280 selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. 

    References: Clin Cancer Res. 2011 Nov 15;17(22):7127-38.

    Related CAS #: 1197376-90-1 (besylate); 1450883-33-6 (fumarate); 1029712-80-8 (free base)  1197376-85-4 (2HCl)  1029714-89-3 (XHCl); 1865733-40-9 (HCl hydrate)

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    Molecular Weight (MW)412.42
    CAS No.1029712-80-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 2 mg/mL (4.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 2-fluoro-N-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide


    InChi Code: InChI=1S/C23H17FN6O/c1-25-22(31)18-6-5-16(11-19(18)24)21-13-28-23-27-12-17(30(23)29-21)10-14-4-7-20-15(9-14)3-2-8-26-20/h2-9,11-13H,10H2,1H3,(H,25,31)

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

    SynonymsCapmatinib; INC280,  INCB 28060; NVP-INC280; INC 280; INCB028060; NVP INC280; INCB28060; INCB-28060; NVPINC280; INC280; INC-280; INCB-028060; INCB 028060; 

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    In Vitro

    In vitro activity: INCB28060 exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10,000-fold selectivity over a large panel of human kinases. INCB28060 inhibits human c-MET phosphorylation and c-MET-mediated signaling in cancer cells. INCB28060 inhibits c-MET-dependent cell proliferation and survival, and prevents anchorage-independent cancer cell growth and cell migration.

    Kinase Assay: The assay buffer contains 50 mM Tris-HCl, 10 mM MgCl2, 100 mM NaCl, 0.1 mg/ml BSA, 5mM DTT, pH 7.8. For HTS 0.8 μL of 5 mM of INCB28060 dissolved in DMSO are dotted on 384-well plates. DMSO titration suggests that the maximum tolerated concentration of the solvent is 4%. To measure IC50s the INCB28060 plate is prepared by 3-fold and 11-point serial dilutions. 0.8 μL of INCB28060 in DMSO is transferred from INCB28060 plate to the assay plate. The final concentration of DMSO is 2%. Solutions of 8 nM unphosphorylated c-Met or 0.5 nM phosphorylated c-Met are prepared in assay buffer. A 1 mM stock solution of peptide substrate Biotin-EQEDEPEGDYFEWLE-amide dissolved in DMSO is diluted to 1 μM in assay buffer containing 400 μM ATP (unphosphorylated c-Met) or 160 uM ATP (phosphorylated c-Met). A 20 μL volume of enzyme solution (or assay buffer for the enzyme blank) is added to the appropriate wells in each plate and then 20 μL/well of substrate solution to initiate the reaction. The plate is protected from light and incubated at 25 °C for 90 minutes. The reaction is stopped by adding 20 μL of a solution containing 45 mM EDTA, 50 mM Tris-HCl, 50 mM NaCl, 0.4 mg/ml BSA, 200 nM SA-APC and 3 nM EUPy20. The plate is incubated for 15-30 minutes at room temperature and HTRF (homogenous time resolved fluorescence) is measured on a Perkin Elmer Fusion α-FP instrument. The HTRF program settings used are as follows: Primary excitation filter 330/30, Primary window: 200 uSec, Primary delay: 50 uSec, Number of flashes: 15, Well read time: 2000.

    Cell Assay: H441 cells are seeded in RPMI-1640 medium containing 10% FBS and grown to complete confluence. Gaps are introduced by scraping cells with a P200 pipette tip. Cells are then stimulated with 50 ng/mL recombinant human HGF to induce migration across the gap in the presence of various concentrations of INCB28060. After an overnight incubation, representative photographs are taken and a semiqualitative assessment of inhibition of cell migration is conducted.

    In VivoINCB28060 shows strong antitumor activity in c-MET-dependent mouse tumor models, even oral treatment of 0.03 mg/kg INCB28060 causes approximately 50% inhibition of c-MET-phosphorylation. Dose-dependent inhibition of tumor growth is observed in tumor-bearing mice. 
    Animal modelEight-week-old female Balb/c nu/nu mice (Charles River) are inoculated subcutaneously with 4 × 106 tumor cells (S114 model) or with 5 × 106 tumor cells (U-87MG glioblastoma model).
    Formulation & DosageDissolved in DMSO; 3, 10, 30 mg/kg; Oral administration.

    Clin Cancer Res. 2011 Nov 15;17(22):7127-38.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Capmatinib (INCB28060)

    INCB28060 inhibits c-MET–dependent cell proliferation and survival. Clin Cancer Res. 2011 Nov 15;17(22):7127-38.

    Capmatinib (INCB28060)

    HGF induces production of TGF-α, AR, and HRG-β1 in cancer cells and INCB28060 effectively blocks the induction.

    Capmatinib (INCB28060)

    Cross-talk between c-MET and EGFR or HER-3 in cancer cells.


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