c-Met-IN-32
c-Met-IN-32 is an orally active c-Met inhibitor with an IC50 of 18 nM, blocking autophosphorylation and downstream PI3K/AKT and RAS/ERK signaling pathways. c-Met-IN-32 inhibits MER, FYN, and SRC kinases. c-Met-IN-32 induces apoptosis, inhibits migration and invasion, suppresses the proliferation of MET-amplified cancer cells, and exhibits selectivity against non-MET-dependent cancer cell lines. c-Met-IN-32 can be used for research on non-small cell lung cancer.
For research use only. We do not sell to patients.
- Formula: C35H36F2N4O6
- Molecular Weight:646.68
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
c-Met 18 nM (IC50) |
PI3K |
Akt |
Ras |
ERK |
Fyn |
MER |
Src |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| EBC-1 | IC50 |
0.12 μM
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Antiproliferative activity against human MET-amplified EBC-1 NSCLC cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human MET-amplified EBC-1 NSCLC cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42748863 |
| A549 | IC50 |
2.5 μM
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Antiproliferative activity against human A549 non-MET-addicted cancer cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human A549 non-MET-addicted cancer cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42748863 |
| HCC827 | IC50 |
2.1 μM
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Antiproliferative activity against human HCC827 non-MET-addicted cancer cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human HCC827 non-MET-addicted cancer cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42748863 |
| HCT-116 | IC50 |
1.8 μM
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Antiproliferative activity against human HCT116 non-MET-addicted cancer cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human HCT116 non-MET-addicted cancer cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42748863 |
| T47D | IC50 |
3.5 μM
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Antiproliferative activity against human T47D non-MET-addicted cancer cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human T47D non-MET-addicted cancer cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42748863 |
| KG-1 | IC50 |
5.2 μM
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Antiproliferative activity against human KG-1 non-MET-addicted cancer cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human KG-1 non-MET-addicted cancer cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42748863 |
| Jurkat | IC50 |
4.0 μM
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Antiproliferative activity against human Jurkat non-MET-addicted cancer cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human Jurkat non-MET-addicted cancer cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42748863 |
| THP-1 | IC50 |
>10 μM
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Antiproliferative activity against human THP-1 non-MET-addicted cancer cells assessed as viability reduction with IC50 greater than 10 μM incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human THP-1 non-MET-addicted cancer cells assessed as viability reduction with IC50 greater than 10 μM incubated 72 hrs by CCK-8 assay.
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42748863 |
In Vitro
c-Met-IN-32 (0.1-10 μM; 2 h) blocks c-Met autophosphorylation and downstream AKT/ERK signaling in EBC-1 cells[1].
c-Met-IN-32 (2-10 nM; 48 h) inhibits EBC-1 cell migration in a concentration-dependent manner at nanomolar concentrations[1].
c-Met-IN-32 (2-10 nM; 24 h) inhibits EBC-1 cell migration and invasion at nanomolar concentrations[1].
c-Met-IN-32 (1 μM) exhibits a more refined kinome profile, with >80% inhibition restricted to MER, FYN, and SRC[1].
c-Met-IN-32 (10 μM) shows moderate Egg-PAMPA permeability, moderate to good liver microsomal stability, and weak inhibition of five major CYP450 isoforms[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EBC-1 cells
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Concentration:0.1, 0.3, 1, 3, and 10 μM
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Incubation Time:2 h
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Result:Produced a concentration-dependent decrease in phosphorylation of c-Met, AKT, and ERK.
p-MET was reduced at 0.1 μM and almost completely abolished at 1 μM and above; p-AKT and p-ERK were substantially suppressed at 0.3 μM.
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Cell Line:EBC-1 cells
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Concentration:50, 100, 200, and 500 nM
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Incubation Time:24 h
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Result:The apoptotic rate increased from 5.2% (DMSO control) to 9.3%, 15.4%, 20.1%, and 24.8% at 50, 100, 200, and 500 nM, respectively.
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Cell Line:EBC-1 cells
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Concentration:2, 5, and 10 nM
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Incubation Time:0, 12, 24, and 48 h
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Result:At 48 h, DMSO control achieved approximately 43% wound closure; compound 41 reduced wound closure to approximately 20% at 2 nM, 16% at 5 nM, and 12% at 10 nM.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 6-8 weeks old)[1]
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Dosage:30 mg/kg
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Administration:p.o.; once daily; 14 days
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Result:Produced a tumor growth inhibition (TGI) rate of 82.2% over the 14-day period.
Chemical Information
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Molecular Weight 646.68
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Formula C35H36F2N4O6
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SMILES
COC1=CC2=C(N=CC=C2OC3=CC=C(NC(C4(CCC4)NC(C5=CC=C(F)C=C5)=O)=O)C=C3F)C=C1OCCCN6CCOCC6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
c-Met-IN-32 Related Classifications
HY-189651 Related Classifications
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