Name: Capmatinib
Brand: Selleck Chemicals
SKU: S2788
Availability: InStock
Rating: 5 (78 reviews)

Chemical Structure

Molecular Weight: 412.42

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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Signaling Pathway

c-Met Signaling Pathway

Cell Culture and Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Mechanism of Action

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. This compound inhibits human c-MET phosphorylation and c-MET-mediated signaling in cancer cells. It 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
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 this compound 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 this chemical 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 this compound. 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 of this compound 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.

References

https://pubmed.ncbi.nlm.nih.gov/21918175/
https://pubmed.ncbi.nlm.nih.gov/30871613/

Chemical Information

Molecular Weight	412.42	Formula	C₂₃H₁₇FN₆O
CAS No.	1029712-80-8	SDF	Download SDF
Synonyms	INC280, NVP-INC280, INCB28060
Smiles	CNC(=O)C1=C(C=C(C=C1)C2=NN3C(=CN=C3N=C2)CC4=CC5=C(C=C4)N=CC=C5)F

Storage and Stability

Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
			1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.300mg/ml (0.73mM)	Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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.

Handling Instructions

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Capmatinib c-Met inhibitor