Capmatinib hydrochloride (Synonyms: INC280 hydrochloride; INCB-28060 hydrochloride)

Cat. No.: HY-13404B Purity: 99.60%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Capmatinib hydrochloride Chemical Structure

CAS No. : 1029714-89-3

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Other In-stock Forms of Capmatinib hydrochloride:

Capmatinib

Other Forms of Capmatinib hydrochloride:

Capmatinib In-stock
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12 Publications Citing Use of MCE Capmatinib hydrochloride

: Capmatinib hydrochloride 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

Formula

C₂₃H₁₈ClFN₆O

CAS No.

1029714-89-3

Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Purity & Documentation

Purity: 99.60%

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Data Sheet (283 KB) SDS (252 KB)

COA (254 KB) HNMR (146 KB) LCMS (94 KB)

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 hydrochloride Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
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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