Capmatinib hydrochloride
Based on 27 publication(s) in Google Scholar
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride 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 hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase.
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- Pureza: 99.48%
- No. CAS: 1029714-89-3
- Fòrmula: C23H18ClFN6O
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Almacenamiento:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Actividad biológica
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Capmatinib hydrochloride
More- Nat Commun. 2026 Jun 4. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Exp Clin Cancer Res. 2022 Sep 16;41(1):275. [Abstract]
- Adv Sci (Weinh). 2025 Jul 17:e00806. [Abstract]
- Leukemia. 2025 Aug 14. [Abstract]
- Int J Biol Macromol. 2024 May;268(Pt 1):131560. [Abstract]
- Clin Transl Med. 2025 May;15(5):e70338. [Abstract]
- Commun Biol. 2022 Nov 26;5(1):1295. [Abstract]
- Int Immunopharmacol. 2021 Feb:91:107287. [Abstract]
- Int J Mol Sci. 2025 Feb 19;26(4):1766. [Abstract]
- Cancer Sci. 2024 May;115(5):1564-1575. [Abstract]
- Biomedicines. 2025 Mar 28;13(4):811. [Abstract]
- Mol Oncol. 2025 Feb;19(2):474-495. [Abstract]
- Cancer Res Treat. 2020 Jul;52(3):973-986. [Abstract]
- Separations. 2023 Apr 10, 10(4), 247.
- Biochem Biophys Rep. 2020 Jan 17;21:100726. [Abstract]
- Biomed Chromatogr. 2024 Oct;38(10):e5986. [Abstract]
- Acta Chromatogr. 2025 Dec 15.
- bioRxiv. 2026 May 5:2026.05.01.722050. [Abstract]
- bioRxiv. 2025 Nov 11.
- Res Sq. 2025 Sep 7.
- bioRxiv. 2025 Jun 7:2025.06.04.657911. [Abstract]
- Research Square Preprint. 2024 Nov 26.
- bioRxiv. 2024 Aug 28:2024.08.27.609975. [Abstract]
- bioRxiv. 2024 Apr 25:2024.04.24.590626. [Abstract]
- Wayne State University. 2014 Jan.
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
Actividad biológica
IC50: 0.13 nM (c-MET)[1]
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.
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Cell Line:SNU-5, S114, H441 and U-87MG
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Concentration:0-10000 nM
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Incubation Time:72 h
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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.
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Cell Line:H441 (stimulated with 50 ng/mL recombinant human HGF for 24h)
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Concentration:0.24, 1, 4, 16 and 63 nM
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Incubation Time:Over night
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Result:Prevented HGF-stimulated H441 cell migration, with IC50 of approximately 2 nM, and less cell migration at 16 nM.
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Cell Line:SNU-5
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Concentration:0.06, 0.24, 0.98, 3.91, 15.63 and 62.25 nM
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Incubation Time:2 h
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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.
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Cell Line:H1993 cells
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Concentration:0.5, 5 and 50 nM
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Incubation Time:20 min
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Result:Suppressed phosphorylation of both EGFR and HER-3 rapidly and as effectively as the compound inhibited c-MET phosphorylation in H1993 cells.
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Cell Line:SNU-5 cells
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Concentration:0.017, 0.15, 1.37, 12.33, 111 and 333 nM
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Incubation Time:24 h
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Result:Effectively induced DNA fragmentation.
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.
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Animal Model:Female Balb/c nu/nu mice (inoculated subcutaneously with 5×106 U-87MG glioblastoma cells)[1]
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Dosage:1, 3, 10 and 30 mg/kg
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Administration:PO, twice daily, for 2 weeks
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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.
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Animal Model:Female Balb/c nu/nu mice (inoculated subcutaneously with 4×106 S114 tumor cells)[1]
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Dosage:0.03, 0.1, 0.3, 1, 3 and 10 mg/kg
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Administration:PO, single dosage
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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.
Chemical Information
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No. CAS 1029714-89-3
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Appearance Solid
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Fòrmula C23H18ClFN6O
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Color Off-white to light yellow
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SMILES
O=C(NC)C1=CC=C(C2=NN3C(N=C2)=NC=C3CC4=CC=C5N=CC=CC5=C4)C=C1F.[x].Cl
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Synonyms
INC280 hydrochloride; INCB-28060 hydrochloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (27)
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Journal Impact Factor
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Most Recent
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Nat Commun
Molecular glue that stabilizes the LRPPRC-MET-G4 interaction complex to drive MET downregulation. [Abstract]2026 Jun 4. PMID: 42243089 -
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 -
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 -
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 hydrochloride 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 hydrochloride 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.
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Leukemia
Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]2025 Aug 14. PMID: 40813622 -
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
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 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 -
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 hydrochloride 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.
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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 -
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 hydrochloride 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 hydrochloride 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).
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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 -
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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 -
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 -
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bioRxiv
2026 May 5:2026.05.01.722050. PMID: 42146489 -
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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 -
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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 -
Capmatinib hydrochloride 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
Pureza y Documentación
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Ficha de datos (283 KB)
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Referencias
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Capmatinib hydrochloride Related Classifications
HY-13404B Related Classifications
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