AM-8735
AM-8735 is a potent and selective MDM2 inhibitor with an IC50 of 25 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 1429386-01-5
- Fòrmula: C27H31Cl2NO6S
- Peso molecular:568.51
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Almacenamiento:
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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Actividad biológica
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Chemical Information
- Protocolo
- Pureza y Documentación
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Help & FAQs
Actividad biológica
IC50: 25 nM (MDM2)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
>25 μM
Compound: 4, AM-8735
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Cytotoxicity against p53-deficient human HCT116 cells assessed as growth inhibition after 16 hrs by flow cytometry-based BrdU incorporation assay in presence of 10% human serum
Cytotoxicity against p53-deficient human HCT116 cells 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: 24548297] |
| HCT-116 | IC50 |
160 nM
Compound: 4, AM-8735
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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 qRT-PCR analysis in presence of 10% human serum
Binding affinity to MDM2 in human HCT116 cells expressing p53 assessed as upregulation of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum
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[PMID: 24548297] |
| HCT-116 | IC50 |
63 nM
Compound: 4, AM-8735
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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: 24548297] |
| SJSA-1 | ED50 |
41 mg/kg
Compound: 4, AM-8735
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Antitumor activity against human SJSA1 cells xenografted in po dosed Harlan athymic nude mouse assessed as tumor growth inhibition administered as qd for 2 weeks measured twice per week
Antitumor activity against human SJSA1 cells xenografted in po dosed Harlan athymic nude mouse assessed as tumor growth inhibition administered as qd for 2 weeks measured twice per week
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[PMID: 24548297] |
| SJSA-1 | IC50 |
25 nM
Compound: 4, AM-8735
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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: 24548297] |
AM-8735 displays substantial growth inhibition of wild-type p53 cells (IC50=63 nM) and no growth inhibition of p53-deficient cells (IC50>25 μM). AM-8735exhibits a dose-dependent increase of p21 mRNA, a direct transcriptional readout of p53 activity, in HCT116 p53wt cells (IC50=160 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1429386-01-5
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Peso molecular 568.51
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Fòrmula C27H31Cl2NO6S
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SMILES
O=C(N1[C@H](CS(=O)(C(C)(C)C)=O)C2CC2)[C@@H](CC(O)=O)O[C@H](C3=CC=CC(Cl)=C3)[C@H]1C4=CC=C(Cl)C=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
SJSA-1 cells cells are treated with AM-8735 for 16 hours in the presence of 10% human serum. Cell proliferation is measured by the Click-iT EdU assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
SJSA-1 cells (5 × 106) are implanted subcutaneously into female athymic nude mice. AM-8735 is administered by oral gavage (as a solution in 15% HPβCD, 1% Pluronic F68, pH 8) 5, 25, 50, and 100 mg/kg q.d. for a period of 2 weeks, and tumor volume is quantified[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AM-8735 Related Classifications
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