1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR

INCB28060 (Synonyms: Capmatinib; INC-280)

Cat. No.: HY-13404 Purity: 99.78%
Handling Instructions

INCB28060 is a potent and selective c-MET kinase inhibitor. INCB28060 inhibits c-MET kinase activity with an average IC50 of 0.13 nM.

For research use only. We do not sell to patients.
INCB28060 Chemical Structure

INCB28060 Chemical Structure

CAS No. : 1029712-80-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 55 In-stock
5 mg USD 50 In-stock
10 mg USD 70 In-stock
50 mg USD 110 In-stock
100 mg USD 150 In-stock
200 mg USD 190 In-stock
500 mg   Get quote  
1 g   Get quote  

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Customer Review

    INCB28060 purchased from MCE. Usage Cited in: Wayne State University. 1-1-2014.

    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
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    INCB28060 is a potent and selective c-MET kinase inhibitor. INCB28060 inhibits c-MET kinase activity with an average IC50 of 0.13 nM.

    IC50 & Target

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

    In Vitro

    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%. INCB28060 inhibits SNU-5 viability or proliferation with an average IC50 value of 1.2 nM and a calculated IC90 value of 4.6 nM INCB28060 prevents HGF-stimulated H441 cell migration, with IC50 of approximately 2 nM. Again, there is little cell migration at a concentration of 16 nM INCB28060. INCB28060 potently and specifically inhibits c-MET enzyme activity, c-MET-mediated signal transduction, and the c-MET-dependent neoplastic phenotype of tumor cells. INCB28060 exhibits strong antitumor activity in c-MET-dependent tumor models at well-tolerated doses. 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 potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis[1].

    In Vivo

    Oral dosing of INCB28060 results in time- and dose-dependent inhibition of c-MET phosphorylation and tumor growth in c-MET-driven mouse tumor models, and the inhibitor is well tolerated at doses that achieve complete tumor inhibition. Furthermore, once daily dosing of 10 mg/kg INCB28060 results in partial regressions in 6 of 10 U-87MG tumor-bearing mice. It is noted that in both S114 and U-87MG models, tumor growth inhibition increases with increased exposure of the compound and that tumor regressions could only be achieved when the compound exposure consistently exceeded 90% of c-MET inhibition. In these studies, INCB28060 is well tolerated at all doses during the treatment periods, with no evidence of overt toxicity or weight loss[1].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.2425 mL 1.2124 mL 2.4247 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    INCB28060 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1].

    Optimal cell density used in the viability assay is predetermined for individual cell lines. To determine compound potency, cells are seeded into 96-well microplates at the appropriate density in media containing 1% to 2% FBS and supplemented with serial dilutions of INCB28060 in a final volume of 100 μL per well. After 72 hour incubation, 24 μL of CellTiter 96 AQueous One Solution is added to each well, and the plates are incubated for 2 hours in a 37°C incubator. The optical density is measured in the linear range using a microplate reader at 490 nm with wavelength correction at 650 nm. IC50 values are calculated using the GraphPad Prism Software[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    INCB28060 is reconstituted in 5% DMAC in 0.5% methylcellulose (Mice)[1].

    Mice[1]
    Tumor-bearing mice are dosed orally, twice each day with 1, 3, 10, or 30 mg/kg of free base INCB28060 reconstituted in 5% DMAC in 0.5% methylcellulose for up to 2 weeks. Body weights are monitored throughout the study as a gross measure of toxicity/morbidity. Tumor growth inhibition, expressed in percent, is calculated using the formula: (1−[(volume (treated)/volume (vehicle)])×100. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    412.42

    Formula

    C₂₃H₁₇FN₆O

    CAS No.

    1029712-80-8

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: 12.66 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.78%

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    Inquiry Information

    Product Name:
    INCB28060
    Cat. No.:
    HY-13404
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