Capmatinib (INCB28060)

For research use only.

Catalog No.S2788 Synonyms: INC280, NVP-INC280

35 publications

Capmatinib (INCB28060) Chemical Structure

CAS No. 1029712-80-8

Capmatinib (INCB28060, INC280, NVP-INC280) is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Capmatinib (INCB28060) inhibits Wnt/β-catenin and EMT signaling pathways and induces apoptosis in diffuse gastric cancer positive for c-MET amplification. Phase 1.

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Selleck's Capmatinib (INCB28060) has been cited by 35 publications

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Biological Activity

Description Capmatinib (INCB28060, INC280, NVP-INC280) is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Capmatinib (INCB28060) inhibits Wnt/β-catenin and EMT signaling pathways and induces apoptosis in diffuse gastric cancer positive for c-MET amplification. Phase 1.
Features Inactive against RONβ, another member of the c-MET RTK family, as well as EGFR and HER-3 (members of the EGFR RTK family).
Targets
Wnt/β-catenin [2]
()		 c-Met [1]
(Cell-free assay)
0.13 nM
In vitro

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. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Huh7-SR NV;ofG81S2WubDD2bYFjcWyrdImgZZN{[Xl? M{nYOVAtKDJuIESsJFgtKDF4IHi= MmD5OFghcA>? NIXZVZd{cWewaX\pZ4FvfGy7IILl[JVk\WRidHjlJJZq[WKrbHn0fUBidmRic4Ty[Y5ofGinbnXkJJRp\SCnZn\lZ5R{KG:oIIPvdoFn\W6rYjDvckB{d3KjZnXubYIuemW|aYP0ZY51KGOnbHzz NUn0UolqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOlQ1OzRpPkK4NVY1PDN2PD;hQi=>
HepG2-SR NH\sS2hE\WyuII\pZYJqdGm2eTDhd5NigQ>? MlrrNEwhOixiNDygPEwhOTZiaB?= M332UVQ5KGh? NH3D[4d{cWewaX\pZ4FvfGy7IILl[JVk\WRidHjlJJZq[WKrbHn0fUBidmRic4Ty[Y5ofGinbnXkJJRp\SCnZn\lZ5R{KG:oIIPvdoFn\W6rYjDvckB{d3KjZnXubYIuemW|aYP0ZY51KGOnbHzz NF[4eWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG2OFQ{PCd-MkixOlQ1OzR:L3G+
NCI-H1993 NFLxRoVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXzweoEyPzJiaILz NGrqO|JIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG5PVMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPDT{05KGG|c3H5MEBKSzVyIE2gNE4xODJ|IN88UU4> NUnncpVzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0NVE1PTVpPkK4OFEyPDV3PD;hQi=>
SNU5 MnTnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnHzO|IhcHK| NYHsW2l{T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hW06XNTDj[YxteyCjZoTldkA4OiCqcoOgZpkhS0ONLUigZZN{[XluIFnDOVAhRSByLkCwNlch|ryPLh?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDRzMUS1OUc,Ojh2MUG0OVU9N2F-

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-Met / Met; 

PubMed: 28164434     


Huh7-SR and HepG2- SR cells were incubated for 48 h with various concentrations of capmatinib and subjected to immunoblotting.

28164434
Immunofluorescence
p-EGFR; 

PubMed: 30390071     


MHCC97-H cells were treated with EGFR inhibitor (10 μM gefitinib), or MET inhibitor (100 nM capmatinib), for 12 hours in serum-free media then fixed and stained for phospho-EGFR. Scale bars are 50μm.

30390071
Growth inhibition assay
Cell viability; 

PubMed: 28164434     


Huh7-SR and HepG2- SR cells were incubated for 48 h with various concentrations of capmatinib and subjected to cell viability assays.

28164434
In vivo

INCB28060 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. [1]

Protocol

Kinase Assay:

[1]
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c-Met 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 Research:

[1]
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  • Cell lines: H441 cells
  • Concentrations: 0.24, 1, 4, 16, 63 nM
  • Incubation Time: 24 hours
  • Method:

    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.


    (Only for Reference)
Animal Research:

[1]
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  • Animal Models: Eight-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).
  • Dosages: 3, 10, 30 mg/kg
  • Administration: INCB28060 is orally dosed, twice each day.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 2 mg/mL (4.84 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 412.42
Formula

C23H17FN6O
CAS No. 1029712-80-8
Storage powder
in solvent
Synonyms INC280, NVP-INC280
Smiles CNC(=O)C1=C(C=C(C=C1)C2=NN3C(=CN=C3N=C2)CC4=CC5=C(C=C4)N=CC=C5)F

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Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID