Capmatinib (INCB28060)

For research use only.

Catalog No.S2788 Synonyms: INC280, NVP-INC280

24 publications

Capmatinib (INCB28060) Chemical Structure

Molecular Weight(MW): 412.42

Capmatinib (INCB28060) 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 24 publications

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Choose Selective c-Met Inhibitors

Biological Activity

Description Capmatinib (INCB28060) 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
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 NXnHPYlGS2WubDD2bYFjcWyrdImgZZN{[Xl? NITjWYgxNCB{LDC0MEA5NCBzNjDo NIXSOZM1QCCq M1nqPJNq\26rZnnjZY51dHlicnXkeYNm\CC2aHWgeoli[mmuaYT5JIFv\CC|dILlcod1cGWwZXSgeIhmKGWoZnXjeJMhd2Zic3;yZYZmdmmkIH;uJJNwemGoZX7pZk1z\XOrc4ThcpQh[2WubIO= NIjzU|EzQDF4NESzOC=>
HepG2-SR NF3V[Y9E\WyuII\pZYJqdGm2eTDhd5NigQ>? M3XpPVAtKDJuIESsJFgtKDF4IHi= NGPBW2s1QCCq M{O2dZNq\26rZnnjZY51dHlicnXkeYNm\CC2aHWgeoli[mmuaYT5JIFv\CC|dILlcod1cGWwZXSgeIhmKGWoZnXjeJMhd2Zic3;yZYZmdmmkIH;uJJNwemGoZX7pZk1z\XOrc4ThcpQh[2WubIO= NXnDRYZiOjhzNkS0N|Q>

... 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=CC=C(C=C1F)C2=N[N]3C(=CN=C3N=C2)CC4=CC=C5N=CC=CC5=C4

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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c-Met Signaling Pathway Map

c-Met Inhibitors with Unique Features

  • Non-specific c-Met Inhibitor

    BMS-777607 : C-Met, IC50=3.9 nM；Axl, IC50=1.1 nM; Ron, IC50=1.8 nM; Tyro3, IC50=4.3 nM.

  • FDA-approved c-Met Inhibitor

    Crizotinib (PF-02341066) : Approved by FDA for non-small cell lung carcinoma (NSCLC).

  • Newest c-Met Inhibitor

    EMD 1214063 New : Potent and selective c-Met inhibitor with IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer.

  • Classic c-Met Inhibitor

    JNJ-38877605 : ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. Phase 1.

Related c-Met Products

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  • Erlotinib New

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  • Bemcentinib（R428) New

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  • Crizotinib (PF-02341066)

    Crizotinib (PF-02341066) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.

  • Foretinib (GSK1363089)

    Foretinib (GSK1363089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.

  • Tivantinib (ARQ 197)

    Tivantinib (ARQ 197) is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Phase 3.

    Features:The first selective c-Met inhibitor to be advanced into human clinical trials.

  • PHA-665752

    PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM in cell-free assays, >50-fold selectivity for c-Met than RTKs or STKs.

  • BMS-777607

    BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases. Phase 1/2.

    Features:A potent inhibitor of the Met family, and >40-fold selectivity vs. Lck, VEGFR2, and TrkA/B and >500-fold selective vs. other receptor and non-receptor kinases.

  • PF-04217903

    PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM in A549 cell line, susceptible to oncogenic mutations (no activity to Y1230C mutant). Phase 1.

  • SU11274

    SU11274 is a selective Met inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID