Cat. No.: HY-13404

Capmatinib

(Synonyms: INC280; INCB28060)

26 Cited Publications

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Based on 26 publication(s) in Google Scholar

Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC₅₀=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase.

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Pureté: 99.71%
CAS No.: 1029712-80-8
Formule: C₂₃H₁₇FN₆O
Masse moléculaire:412.42

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Capmatinib Chemical Structure

CAS No.: 1029712-80-8

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (26)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

c-Met

Cellular Effect

Cell Line	Type	Value	Description	References
EBC-1	IC₅₀	1.2 nM Compound: Capmatinib	Antiproliferative activity against human EBC-1 cells Antiproliferative activity against human EBC-1 cells	[PMID: 38169272]
NCI-H1993	IC₅₀	2.3 nM Compound: INCB28060	Growth inhibition of human NCI-H1993 cells after 72 hrs by CCK-8 assay Growth inhibition of human NCI-H1993 cells after 72 hrs by CCK-8 assay	[PMID: 28411455]
SNU-5	IC₅₀	2.7 nM Compound: INCB28060	Growth inhibition of human SNU5 cells after 72 hrs by CCK-8 assay Growth inhibition of human SNU5 cells after 72 hrs by CCK-8 assay	[PMID: 28411455]

In Vitro

Capmatinib (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%, which is reversible and the effect is significantly reduced in several hours after the compound is removed and completely disappeared by 48 hours^[1].
Capmatinib (INCB28060) (0-10000 nM; 72 h) inhibits the proliferation of SNU-5, S114, H441 and U-87MG^[1].
Capmatinib (INCB28060) (0.06-62.25 nM; 2h) effectively inhibits phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5^[1].
Capmatinib (INCB28060) (0.24-63 nM; over night) prevents HGF-stimulated H441 cell migration^[1].
Capmatinib (INCB28060) (0.5-50 nM; 20 min) suppresses phosphorylation of both EGFR and HER-3 rapidly^[1].
Capmatinib (INCB28060) (0-333 nM; 24 h) induces apoptosis in SNU-5 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

SNU-5, S114, H441 and U-87MG
Concentration:

0-10000 nM
Incubation Time:

72 h
Result:

Inhibited the cell viability of SNU-5 and S114, as well as the colony formation of H441 and U-87MG, with IC₅₀ values of 1.2 nM, 12.4 nM, ~0.5 nM and 2 nM, respectively.

Cell Migration Assay ^[1]

Cell Line:

H441 (stimulated with 50 ng/mL recombinant human HGF for 24h)
Concentration:

0.24, 1, 4, 16 and 63 nM
Incubation Time:

Over night
Result:

Prevented HGF-stimulated H441 cell migration, with IC₅₀ of approximately 2 nM, and less cell migration at 16 nM.

Western Blot Analysis^[1]

Cell Line:

SNU-5
Concentration:

0.06, 0.24, 0.98, 3.91, 15.63 and 62.25 nM
Incubation Time:

2 h
Result:

Effectively inhibited phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5.

Western Blot Analysis^[1]

Cell Line:

H1993 cells
Concentration:

0.5, 5 and 50 nM
Incubation Time:

20 min
Result:

Suppressed phosphorylation of both EGFR and HER-3 rapidly and as effectively as the compound inhibited c-MET phosphorylation in H1993 cells.

Apoptosis Analysis^[1]

Cell Line:

SNU-5 cells
Concentration:

0.017, 0.15, 1.37, 12.33, 111 and 333 nM
Incubation Time:

24 h
Result:

Effectively induced DNA fragmentation.

In Vivo

Capmatinib (INCB28060) (1-30 mg/kg; PO, twice daily, for 2 weeks) exhibits dose-dependent inhibition of tumor growth, and shows well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss in U-87MG tumor mice model^[1].
Capmatinib (INCB28060) (0.03-10 mg/kg; PO, single dosage) causes inhibition of c-MET phosphorylation in S114 tumor mice model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female Balb/c nu/nu mice (inoculated subcutaneously with 5×10⁶ U-87MG glioblastoma cells)^[1]
Dosage:

1, 3, 10 and 30 mg/kg
Administration:

PO, twice daily, for 2 weeks
Result:

Exhibited dose-dependent inhibition of tumor growth with 35% and 76% at 1 and 3 mg/kg once daily; resulted in partial regressions in 6 of 10 U-87MG tumor-bearing mice at 10 mg/kg once daily; and showed well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss.

Animal Model:

Female Balb/c nu/nu mice (inoculated subcutaneously with 4×10⁶ S114 tumor cells)^[1]
Dosage:

0.03, 0.1, 0.3, 1, 3 and 10 mg/kg
Administration:

PO, single dosage
Result:

Caused approximately 50% and 90% inhibition of c-MET phosphorylation at 0.03 and 0.3 mg/kg after administration of 30 min, and inhibition of phospho-c-MET exceeded 90% after 7 hours.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1029712-80-8
Appearance Solid
Masse moléculaire 412.42
Formule C₂₃H₁₇FN₆O
Color Light yellow to yellow
SMILES

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

INC280; INCB28060
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (26)

All In Vivo Efficacy StudyCell Proliferation/Viability AssayWB

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Adv Sci (Weinh)

The Evolutionary Trajectory and Prognostic Value of GITR+ Tregs Reprogramed by Tumor-Intrinsic PD-1/c-MET Signaling in Pancreatic Cancer. [Abstract]

2025 Jul 17:e00806. PMID: 40673866

Capmatinib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 17:e00806. [Abstract]

A) Orthotopic inoculated KPC tumors from the control, Capmatinib (INC280) monotherapy, DTA-1 monotherapy and combined therapy groups. B) Quantification of tumor weights under different treatment.Male C57BL/6 mice (KPC cells，orthotopic pancreatic tumor model ), 1) vehicle (5% DMSO + 45% PEG300/5% Tween80 + 50% ddH2O) + IgG control, 2) MET inhibitor monotherapy: INC280 (10 mg kg day−1 for 8 days) + IgG, 3) GITR agonist monotherapy: DTA‐1 (100 µg mouse day−1 for 4 days) + vehicle, and 4) combination therapy: INC280+ DTA‐1. INC280 was formulated in a vehicle solution of DMSO/PEG300/Tween80/ddH₂O (5:45:5:50, v/v) and administered by intraperitoneal injection.

Capmatinib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 17:e00806. [Abstract]

Flowcytometry analysis of GzmB , and TNF-α expression in CD8+ T cells under different treatment. Male C57BL/6 mice (KPC cells，orthotopic pancreatic tumor model ), 1) vehicle (5% DMSO + 45% PEG300/5% Tween80 + 50% ddH2O) + IgG control, 2) MET inhibitor monotherapy: INC280 (Capmatinib, 10 mg kg day−1 for 8 days) + IgG, 3) GITR agonist monotherapy: DTA‐1 (100 µg mouse day−1 for 4 days) + vehicle, and 4) combination therapy: INC280+ DTA‐1. INC280 was formulated in a vehicle solution of DMSO/PEG300/Tween80/ddH₂O (5:45:5:50, v/v) and administered by intraperitoneal injection.
Leukemia

Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]

2025 Aug 14. PMID: 40813622
J Exp Clin Cancer Res

HGF-mediated elevation of ETV1 facilitates hepatocellular carcinoma metastasis through upregulating PTK2 and c-MET. [Abstract]

2022 Sep 16;41(1):275. PMID: 36109787
Int J Biol Macromol

Exploring the association of POSTN+ cancer-associated fibroblasts with triple-negative breast cancer. [Abstract]

2024 May;268(Pt 1):131560. PMID: 38631570
Clin Transl Med

Responsiveness of different MET tumour alterations to type I and type II MET inhibitors. [Abstract]

2025 May;15(5):e70338. PMID: 40437874
Commun Biol

A pipeline for malignancy and therapy agnostic assessment of cancer drug response using cell mass measurements. [Abstract]

2022 Nov 26;5(1):1295. PMID: 36435843
Int J Mol Sci

Application of an Integrated Single-Cell and Three-Dimensional Spheroid Culture Platform for Investigating Drug Resistance Heterogeneity and Epithelial-Mesenchymal Transition (EMT) in Lung Cancer Subclones. [Abstract]

2025 Feb 19;26(4):1766. PMID: 40004228

Capmatinib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Feb 19;26(4):1766. [Abstract]

In the 3D culture system, MPE primary cells formed stable spheroids within 96 h. Drug sensitivity assays using the 3D tumorsphere model showed that Giotrif (afatinib) at 60 nM and Capmatinib (0.8 nM; 96 h) at 6.5 nM achieved IC50.
Int Immunopharmacol

Natterin an aerolysin-like fish toxin drives IL-1β-dependent neutrophilic inflammation mediated by caspase-1 and caspase-11 activated by the inflammasome sensor NLRP6. [Abstract]

2021 Feb:91:107287. PMID: 33378723
Mol Oncol

Functional interaction between receptor tyrosine kinase MET and ETS transcription factors promotes prostate cancer progression. [Abstract]

2025 Feb;19(2):474-495. PMID: 39374163

Capmatinib purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2025 Feb;19(2):474-495. [Abstract]

Capmatinib (0.5,1 μM; 24 h) toxicity was also tested through MTT tests at higher concentration.

Capmatinib purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2025 Feb;19(2):474-495. [Abstract]

(A)Graphical representation of tumour volume over time after subcutaneous injection of PC3M Ctrl, PC3M ETV1 and PC3M ERG cells. The tumour volume of the mice was monitored by palpation. (B) Graphical representation of the final tumour volume of mice having been treated or not with Capmatinib.8‐week‐old male NSG‐hHGFki mice (PC3M cells), Capmatinib (10 mg/kg; oral gavage 5 days a week, 30 days).
Cancer Sci

Gap junction beta-4 accelerates cell cycle progression and metastasis through MET-AKT activation in pancreatic cancer. [Abstract]

2024 May;115(5):1564-1575. PMID: 38342100
Biomedicines

Phosphorylation of MET Is Upregulated in Metastatic Sites of Renal Cell Carcinoma: Possible Role of MET and Hepatocyte Growth Factor Activation-Targeted Combined Therapy. [Abstract]

2025 Mar 28;13(4):811. PMID: 40299443
Cancer Res Treat

RON and MET Co-overexpression Are Significant Pathological Characteristics of Poor Survival and Therapeutic Targets of Tyrosine Kinase Inhibitors in Triple-Negative Breast Cancer. [Abstract]

2020 Jul;52(3):973-986. PMID: 32324988
Separations

2023 Apr 10, 10(4), 247.
Biochem Biophys Rep

Cabozantinib inhibits AXL- and MET-dependent cancer cell migration induced by growth-arrest-specific 6 and hepatocyte growth factor. [Abstract]

2020 Jan 17;21:100726. PMID: 32055714
Acta Chromatogr

2025 Dec 15.
Biomed Chromatogr

Development and validation of an ultra-performance liquid chromatography-tandem mass spectrometry method to quantify the small molecule inhibitors adagrasib, alectinib, brigatinib, capmatinib, crizotinib, lorlatinib, selpercatinib, and sotorasib in human plasma. [Abstract]

2024 Oct;38(10):e5986. PMID: 39136165
bioRxiv

Met regulates endoderm migration in zebrafish. [Abstract]

2026 May 5:2026.05.01.722050. PMID: 42146489
bioRxiv

2025 Nov 11.
Res Sq

2025 Sep 7.
bioRxiv

Modeling acquired TKI resistance and effective combination therapeutic strategies in murine RET+ lung adenocarcinoma. [Abstract]

2025 Jun 7:2025.06.04.657911. PMID: 40502048
Research Square Preprint

2024 Nov 26.
bioRxiv

Cancer-associated fibroblasts confer ALK inhibitor resistance in EML4-ALK -driven lung cancer via concurrent integrin and MET signaling. [Abstract]

2024 Aug 28:2024.08.27.609975. PMID: 39253447
bioRxiv

Peristromal niches protect lung cancers from targeted therapies through a combined effect of multiple molecular mediators. [Abstract]

2024 Apr 25:2024.04.24.590626. PMID: 38712093
Wayne State University

2014 Jan.

Capmatinib purchased from MedChemExpress. Usage Cited in: Wayne State University. 2014 Jan.

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

Solvant et solubilité

In Vitro:

DMSO : 5 mg/mL (12.12 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water

Solubility: 10 mg/mL (24.25 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (293 KB)
SDS (396 KB)
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- Swedish - SV (396 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Liu X, et al. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clin Cancer Res. 2011 Nov 15;17(22):7127-38. [Content Brief]

[2]. Baltschukat S, et al. Capmatinib (INC280) Is Active Against Models of Non-Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation. Clin Cancer Res. 2019 May 15;25(10):3164-3175. [Content Brief]

[3]. Dhillon S. Capmatinib: First Approval. Drugs. 2020 Jul;80(11):1125-1131. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4247 mL	12.1236 mL	24.2471 mL	60.6178 mL
	5 mM	0.4849 mL	2.4247 mL	4.8494 mL	12.1236 mL
	10 mM	0.2425 mL	1.2124 mL	2.4247 mL	6.0618 mL

Capmatinib

26 Cited Publications

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Capmatinib

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Publications Citing Use of MedChemExpress (MCE) Capmatinib

Activité biologique

Chemical Information

Publications (26)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Capmatinib Related Classifications

Cat. No.: HY-13404