1. Apoptosis
  2. MDM-2/p53
  3. AMG 232

AMG 232 

Cat. No.: HY-12296 Purity: 99.90%
Handling Instructions

AMG 232 is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. AMG 232 binds to MDM2 with a Kd of 0.045 nM.

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

AMG 232 Chemical Structure

AMG 232 Chemical Structure

CAS No. : 1352066-68-2

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Based on 1 publication(s) in Google Scholar

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Description

AMG 232 is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. AMG 232 binds to MDM2 with a Kd of 0.045 nM.

IC50 & Target

IC50: 0.6 nM (p53-MDM2 interaction)[1]
Kd: 0.045 nM (MDM2)[1]

In Vitro

AMG 232 (10 μM) induces p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines[1].
AMG 232 potently inhibits proliferation of non-MDM2-amplified HCT116 colorectal cells (IC50=10 nM)[3].

Cell Viability Assay[1]

Cell Line: SJSA-1, HCT116, ACHN, NCI-H460, MOLM-13, RKO, MCF7, 22RV1, HT-29, PC-3, NCI-H82, NCI-SNU1, MG-63, NCI-H2452, SW982, C32, SK-HEP-1, A375, RT4, RPMI2650, MDA-MB-134-VI, NCI-H2347 and A427 cells.
Concentration: 0-10 μM.
Incubation Time: 72 hours.
Result: Induced p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines (SJSA-1, HCT116, and ACHN).
Caused robust p21 mRNA induction between 9.76 and 34.9 fold with IC50 values ranging from 12.8 to 46.8 nM.
In Vivo

AMG 232 (10, 25, 75 mg/kg, once daily, p.o.) activates p53 pathway activity in vivo[1].
AMG 232 (10, 25, 75 mg/kg, once daily, p.o.) potently inhibits growth of tumor xenografts in mice[1].
AMG 232 (10, 25, 75 mg/kg, once daily, p.o.) blocks DNA synthesis and induces apoptosis in vivo[1].
AMG 232 causes a dose-dependent tumor growth inhibition with an ED50 of 16 mg/kg[2].

Animal Model: Female athymic nude mice (n=10/group) based cancer models[1].
Dosage: 10, 25, 75 mg/kg.
Administration: Once daily by oral gavage.
Result: Resulted in significant tumor growth inhibition across all models. SJSA-1, an MDM2 amplified osteosarcoma model, was the most sensitive to AMG 232 treatment with an ED50 of 9.1 mg/kg. In the highest dose group of 75 mg/kg, 10/10 tumors completely regressed and were undetectable after 10 days of treatment.
Clinical Trial
Molecular Weight

568.55

Formula

C₂₈H₃₅Cl₂NO₅S

CAS No.

1352066-68-2

SMILES

O=C(O)C[[email protected]]1(C)C(N([[email protected]](CS(=O)(C(C)C)=O)C(C)C)[[email protected]](C2=CC=C(Cl)C=C2)[[email protected]@H](C3=CC=CC(Cl)=C3)C1)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (87.94 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7589 mL 8.7943 mL 17.5886 mL
5 mM 0.3518 mL 1.7589 mL 3.5177 mL
10 mM 0.1759 mL 0.8794 mL 1.7589 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.90%

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