AM-8553
AM-8553 is a MDM2/p53 inhibitor (KD: 0.4 nM for MDM2). AM-8553 has anti-tumor activity
For research use only. We do not sell to patients.
- CAS No.: 1352064-70-0
- Formula: C25H29Cl2NO4
- Molecular Weight:478.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
>25 μM
Compound: 29, AM-8553
|
Antiproliferative activity against p53 deficient human HCT116 cells assessed as reduction in BrdU incorporation after 16 hrs by Flow cytometry
Antiproliferative activity against p53 deficient human HCT116 cells assessed as reduction in BrdU incorporation after 16 hrs by Flow cytometry
|
[PMID: 22524527] |
| HCT-116 | IC50 |
0.2 μM
Compound: 29, AM-8553
|
Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as reduction in BrdU incorporation after 16 hrs by Flow cytometry
Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as reduction in BrdU incorporation after 16 hrs by Flow cytometry
|
[PMID: 22524527] |
| SJSA-1 | ED50 |
78 mg/kg
Compound: 29, AM-8553
|
Antitumor activity against human SJSA1 cells xenografted in po dosed athymic nude mouse assessed as tumor growth inhibition administered qd after 14 days
Antitumor activity against human SJSA1 cells xenografted in po dosed athymic nude mouse assessed as tumor growth inhibition administered qd after 14 days
|
[PMID: 22524527] |
| SJSA-1 | IC50 |
0.068 μM
Compound: 29, AM-8553
|
Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation assay in presence of 10% human serum
Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation assay in presence of 10% human serum
|
[PMID: 22524527] |
| SJSA-1 | IC50 |
0.073 μM
Compound: 1, AM-8553
|
Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation-based HCS assay in presence of 10% human serum
Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation-based HCS assay in presence of 10% human serum
|
[PMID: 25147610] |
| SJSA-1 | IC50 |
0.76 μM
Compound: 29, AM-8553
|
Activity at p53 in human SJSA1 cells assessed as induction of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum
Activity at p53 in human SJSA1 cells assessed as induction of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum
|
[PMID: 22524527] |
| SJSA-1 | IC50 |
72 nM
Compound: 1, AM-8553
|
Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum
Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum
|
[PMID: 24456472] |
| SJSA-1 | IC50 |
760 nM
Compound: 1, AM-8553
|
Antiproliferative activity against human SJSA1 cells assessed as induction of p21 gene level by qRT-PCR assay in presence of 10% human serum
Antiproliferative activity against human SJSA1 cells assessed as induction of p21 gene level by qRT-PCR assay in presence of 10% human serum
|
[PMID: 24456472] |
Chemical Information
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CAS No. 1352064-70-0
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Molecular Weight 478.41
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Formula C25H29Cl2NO4
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SMILES
O=C(O)C[C@]1(C)C(N([C@@H](CC)[C@@H](O)C)[C@H](C2=CC=C(Cl)C=C2)[C@@H](C3=CC=CC(Cl)=C3)C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)