AM-8553

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AM-8553 is a MDM2/p53 inhibitor (K_D: 0.4 nM for MDM2). AM-8553 has anti-tumor activity

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AM-8553 Chemical Structure

CAS No. : 1352064-70-0

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Description

AM-8553 is a MDM2/p53 inhibitor (K_D: 0.4 nM for MDM2). AM-8553 has anti-tumor activity^[1]

Cellular Effect

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	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]
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]

Molecular Weight

478.41

Formula

C₂₅H₂₉Cl₂NO₄

CAS No.

1352064-70-0

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Bernard D, et al. AM-8553: a novel MDM2 inhibitor with a promising outlook for potential clinical development. J Med Chem. 2012 Jun 14;55(11):4934-5. [Content Brief]

AM-8553 Related Classifications

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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	×		=		×
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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AM-85531352064-70-0AM8553AM 8553MDM-2/p53SJSA-1 xenograft tumorMDM2/p53Inhibitorinhibitorinhibit

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