AM-6761
AM-6761 is a potent MDM2 inhibitor with an IC50 of 0.1 nM.
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- CAS No.: 1584732-36-4
- Formule: C33H37Cl2FN2O5S2
- Masse moléculaire:695.69
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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
IC50: 0.1 nM (MDM2)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
11 nM
Compound: 4, AM-6761
|
Cytotoxicity against human HCT116 cells expressing p53 assessed as growth inhibition after 16 hrs by flow cytometry-based BrdU incorporation assay in presence of 10% human serum
Cytotoxicity against human HCT116 cells expressing p53 assessed as growth inhibition after 16 hrs by flow cytometry-based BrdU incorporation assay in presence of 10% human serum
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[PMID: 24601644] |
| HCT-116 | IC50 |
58 nM
Compound: 4, AM-6761
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Binding affinity to MDM2 in human HCT116 cells expressing p53 assessed as upregulation of p21 mRNA expression after 7 hrs by quantitative RT-PCR analysis
Binding affinity to MDM2 in human HCT116 cells expressing p53 assessed as upregulation of p21 mRNA expression after 7 hrs by quantitative RT-PCR analysis
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[PMID: 24601644] |
| SJSA-1 | ED50 |
11 mg/kg
Compound: 4, AM-6761
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Antitumor activity against human SJSA1 cells xenografted in po dosed Harlan athymic nude mouse assessed as tumor growth inhibition at 25 mg/kg, administered as qd on day 9 post tumor implantation measured twice per week
Antitumor activity against human SJSA1 cells xenografted in po dosed Harlan athymic nude mouse assessed as tumor growth inhibition at 25 mg/kg, administered as qd on day 9 post tumor implantation measured twice per week
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[PMID: 24601644] |
| SJSA-1 | IC50 |
16 nM
Compound: 4, AM-6761
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Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum
Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum
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[PMID: 24601644] |
In Vitro
AM-6761 is a potent inhibitor with remarkable biochemical (IC50=0.1 nM) and cellular potency (IC50=16 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1584732-36-4
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Masse moléculaire 695.69
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Formule C33H37Cl2FN2O5S2
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SMILES
O=C(O)CC1=CN=C(C[C@]2(C)C(N([C@@H](C3CC3)CS(=O)(C(C)(C)C)=O)[C@H](C4=CC=C(Cl)C(F)=C4)[C@@H](C5=CC=CC(Cl)=C5)C2)=O)S1
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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)
AM-6761 Related Classifications
HY-12737 Related Classifications
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