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> Capmatinib [1029712-80-8]

Capmatinib [1029712-80-8]

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Référence HY-13404-5mg

Conditionnement : 5mg

Marque : MedChemExpress

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Description

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[1][2][3].

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.

Capmatinib Related Antibodies

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
Masse moléculaire

412.42

Formule

C23H17FN6O
CAS No.
Appearance

Solid

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
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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4247 mL 12.1236 mL 24.2471 mL
5 mM 0.4849 mL 2.4247 mL 4.8494 mL
View the Complete Stock Solution Preparation Table

* 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.

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureté et documentation
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