c-Met degrader-1
c-Met degrader-1 is an orally active c-Met HyT degrader with a DC50 of 226.12 nM. c-Met degrader-1 exhibits anticancer activity against hepatocellular carcinoma. c-Met degrader-1 can be used in the research of hepatocellular carcinoma (HCC) (c-Met ligand: Tepotinib (HY-14721), hydrophobic tag moiety: Adamantan-1-ylmethanamine (HY-W037848)).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C45H53N7O3
- Masse moléculaire:739.95
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
c-Met 226.12 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MHCC97H | IC50 |
2.62 nM
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Antiproliferative activity against human MHCC97H hepatocellular carcinoma cells, quantified as the half-maximal inhibitory concentration for cell proliferation.
Antiproliferative activity against human MHCC97H hepatocellular carcinoma cells, quantified as the half-maximal inhibitory concentration for cell proliferation.
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38962837 |
| MHCC97H | DC50 |
226.12 nM
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c-Met protein degradation activity in human MHCC97H hepatocellular carcinoma cells, quantified as the half-maximal degradation concentration after 24 h incubation.
c-Met protein degradation activity in human MHCC97H hepatocellular carcinoma cells, quantified as the half-maximal degradation concentration after 24 h incubation.
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38962837 |
In Vitro
c-Met degrader-1 (63-1000 nM; 24 h) degrades c-Met protein in MHCC97H cells in a concentration-dependent manner with a DC50 of 226.12 nM[1].
c-Met degrader-1 (500 nM; 3-48 h) degrades c-Met protein in MHCC97H cells in a time-dependent manner, with near-complete degradation achieved by 24 h[1].
c-Met degrader-1 (63-1000 nM; 24 h) degrades c-Met protein in HuH7 cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MHCC97H human hepatocellular carcinoma cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Inhibited proliferation of MHCC97H cells with an IC50 of 2.62 nM.
Degraded 84.77% of c-Met protein in MHCC97H cells.
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 mice (6 mice per group)[1]
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Dosage:10 mg/kg (TGI 61.5%); 20 mg/kg (TGI 52.5%)
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Administration:i.p.; daily; 22 days; p.o.; daily; 22 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 52.5%.
Achieved a tumor growth inhibition (TGI) rate of 61.5%.
Downregulated c-Met, phospho-c-Met, and phospho-STAT3 protein levels significantly in tumor tissues.
Showed no lesions in major organs via H&E staining.
Caused no significant body weight differences between treated and control groups.
Reduced tumor cell proliferation, with the i.p. group exhibiting the lowest tumor positive rate via Ki67 staining.
Chemical Information
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Masse moléculaire 739.95
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Formule C45H53N7O3
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SMILES
O=C1C=CC(C2=CC(C#N)=CC=C2)=NN1CC3=CC(C4=NC=C(C=N4)OCC5CCN(CC5)CCCCCC(NCC67C[C@@H](C[C@@H](C7)C8)C[C@@H]8C6)=O)=CC=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
c-Met degrader-1 Related Classifications
HY-162679 Related Classifications
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