Capmatinib dihydrochloride (Synonyms: INC280 dihydrochloride; INCB28060 dihydrochloride)

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Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC₅₀=0.13 nM). Capmatinib dihydrochloride 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 dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase.

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Capmatinib dihydrochloride Chemical Structure

CAS No. : 1197376-85-4

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Other In-stock Forms of Capmatinib dihydrochloride:

Capmatinib

Other Forms of Capmatinib dihydrochloride:

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12 Publications Citing Use of MCE Capmatinib dihydrochloride

: Capmatinib dihydrochloride purchased from MedChemExpress. Usage Cited in: Department Cancer Biology. 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

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Description

IC₅₀ & Target

IC₅₀: 0.13 nM (c-MET)^[1]

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.

Clinical Trial

Molecular Weight

485.34

Formula

C₂₃H₁₉Cl₂FN₆O

CAS No.

1197376-85-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

Capmatinib dihydrochloride Related Classifications

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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