Home Protein Tyrosine Kinase c-Met inhibitor - Wnt/beta-catenin inhibitor - Apoptosis related activator Capmatinib For research use only.

Capmatinib

Synonyms: INC280, NVP-INC280, INCB28060

Capmatinib 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.

Capmatinib Chemical Structure

Capmatinib Chemical Structure

CAS: 1029712-80-8

Selleck's Capmatinib has been cited by 73 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Huh7-SR Cell viability assay 0, 2, 4, 8, 16 h 48 h significantly reduced the viability and strengthened the effects of sorafenib on sorafenib-resistant cells 28164434
HepG2-SR Cell viability assay 0, 2, 4, 8, 16 h 48 h significantly reduced the viability and strengthened the effects of sorafenib on sorafenib-resistant cells 28164434
NCI-H1993 Growth inhibition assay 72 hrs Growth inhibition of human NCI-H1993 cells after 72 hrs by CCK-8 assay, IC50 = 0.0023 μM. 28411455
SNU5 Growth inhibition assay 72 hrs Growth inhibition of human SNU5 cells after 72 hrs by CCK-8 assay, IC50 = 0.0027 μM. 28411455
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Biological Activity

Description Capmatinib 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
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]
Kinase Assay 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 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-Met / Met 28164434
Immunofluorescence p-EGFR 30390071
Growth inhibition assay Cell viability 28164434
In Vivo
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]
Animal Research 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.

Chemical lnformation & Solubility

Molecular Weight 412.42 Formula

C23H17FN6O
CAS No. 1029712-80-8 SDF Download Capmatinib SDF
Smiles CNC(=O)C1=C(C=C(C=C1)C2=NN3C(=CN=C3N=C2)CC4=CC5=C(C=C4)N=CC=C5)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 6 mg/mL ( (14.54 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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