1. Apoptosis
    Metabolic Enzyme/Protease
  2. MDM-2/p53
    E1/E2/E3 Enzyme
  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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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    AMG 232 purchased from MCE. Usage Cited in: Cell Death Discov. 2020 Jul.

    The effect of AMG-232 on the p53 signaling pathway, and the expression of IL-6 and PD-L1 at different drug doses is assessed by immunoblotting. AMG-232 treatment leads to activation of the p53 signaling pathway in the cancer cells in a dose-dependent manner. The effect of significant reduction in IL-6 expression is observed with AMG-232 in a dose-dependent manner.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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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    Keywords:

    AMG 232AMG232AMG-232MDM-2/p53E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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    Product Name:
    AMG 232
    Cat. No.:
    HY-12296
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