AM-8735

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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.

AM-8735 Chemical Structure

CAS No. : 1429386-01-5

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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	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]
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]

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.

Molecular Weight

568.51

Formula

C₂₇H₃₁Cl₂NO₆S

CAS No.

1429386-01-5

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

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]

Cell Assay ^[1]	SJSA-1 cells cells are treated with AM-8735 for 16 hours in the presence of 10% human serum. Cell proliferation is measured by the Click-iT EdU assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Rats^[1] SJSA-1 cells (5 × 10⁶) are implanted subcutaneously into female athymic nude mice. AM-8735 is administered by oral gavage (as a solution in 15% HPβCD, 1% Pluronic F68, pH 8) 5, 25, 50, and 100 mg/kg q.d. for a period of 2 weeks, and tumor volume is quantified^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]

AM-8735 Related Classifications

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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-87351429386-01-5AM8735AM 8735MDM-2/p53E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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