AM-6761
AM-6761 is a potent MDM2 inhibitor with an IC50 of 0.1 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 1584732-36-4
- Fòrmula: C33H37Cl2FN2O5S2
- Peso molecular:695.69
-
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]
-
Actividad biológica
-
Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
IC50: 0.1 nM (MDM2)[1]
|
Cell Line
|
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
|
[PMID: 24601644] |
| HCT-116 | IC50 |
58 nM
Compound: 4, AM-6761
|
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
|
[PMID: 24601644] |
| SJSA-1 | ED50 |
11 mg/kg
Compound: 4, AM-6761
|
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
|
[PMID: 24601644] |
| SJSA-1 | IC50 |
16 nM
Compound: 4, AM-6761
|
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
|
[PMID: 24601644] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 1584732-36-4
-
Peso molecular 695.69
-
Fòrmula C33H37Cl2FN2O5S2
-
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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
HCT116 cells are treated with AM-6761 (0.001-10 μM). The potency of MDM2 inhibitors is determined byBrdU proliferation assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
SJSA-1 cells (5 × 106) are implanted subcutaneously into female athymic nude mice. Treatment with vehicle or 4 at 5, 12.5, 25, or 50 mg/kg QD AM-6761 by oral gavage begins on day 9 when tumors reach 200 mm3. Tumor sizes and body weights are measured twice per week[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-6761 Related Classifications
HY-12737 Related Classifications
Powered by Bioz