1. Apoptosis
  2. MDM-2/p53

AM-8735 

Cat. No.: HY-12734
Handling Instructions

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

AM-8735 Chemical Structure

CAS No. : 1429386-01-5

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 25 nM (MDM2)[1]

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].

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7590 mL 8.7949 mL 17.5898 mL
5 mM 0.3518 mL 1.7590 mL 3.5180 mL
10 mM 0.1759 mL 0.8795 mL 1.7590 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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
Molecular Weight

568.51

Formula

C₂₇H₃₁Cl₂NO₆S

CAS No.

1429386-01-5

SMILES

O=C(N1[[email protected]](CS(=O)(C(C)(C)C)=O)C2CC2)[[email protected]@H](CC(O)=O)O[[email protected]](C3=CC=CC(Cl)=C3)[[email protected]]1C4=CC=C(Cl)C=C4

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
AM-8735
Cat. No.:
HY-12734
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AM-8735

Cat. No.: HY-12734