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Cat. No.: HY-12734

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AM-8735

AM-8735 is a potent and selective MDM2 inhibitor with an IC₅₀ of 25 nM.

For research use only. We do not sell to patients.

CAS No.: 1429386-01-5
Formula: C₂₇H₃₁Cl₂NO₆S
Molecular Weight:568.51

Storage:

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

Data Sheet (280 KB)

AM-8735 Chemical Structure

CAS No.: 1429386-01-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

AM-8735 is a potent and selective MDM2 inhibitor with an IC₅₀ of 25 nM.

IC₅₀ & Target

IC50: 25 nM (MDM2)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	>25 μM Compound: 4, AM-8735	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	[PMID: 24548297]
HCT-116	IC₅₀	160 nM Compound: 4, AM-8735	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	[PMID: 24548297]
HCT-116	IC₅₀	63 nM Compound: 4, AM-8735	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: 24548297]
SJSA-1	ED₅₀	41 mg/kg Compound: 4, AM-8735	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	[PMID: 24548297]
SJSA-1	IC₅₀	25 nM Compound: 4, AM-8735	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: 24548297]

In Vitro

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. .

In Vivo

AM-8735 also demonstrates significant time and concentration dependent p21 mRNA induction in vivo in a pharmacodynamic assay in SJSA-1 osteosarcoma tumors. AM-8735 shows excellent antitumor activity in the SJSA-1 osteosarcoma xenograft model with an ED₅₀ of 41 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1429386-01-5
Molecular Weight 568.51
Formula C₂₇H₃₁Cl₂NO₆S
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
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Gonzalez AZ, et al. Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction. J Med Chem. 2014 Mar 27;57(6):2472-88. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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