AM-6761
AM-6761 is a potent MDM2 inhibitor with an IC50 of 0.1 nM.
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- CAS 番号: 1584732-36-4
- 分子式: C33H37Cl2FN2O5S2
- 分子量:695.69
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
IC50: 0.1 nM (MDM2)[1]
Cellular Effect
|
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] |
体外実験
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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
-
CAS 番号 1584732-36-4
-
分子量 695.69
-
分子式 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
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)