An inhibitor of the MDM2 and p53 interaction
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AMG 232

Item No. 25667

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-3-methyl-1-[(1S)-2-methyl-1-[[(1-methylethyl)sulfonyl]methyl]propyl]-2-oxo-3-piperidineacetic acid
CAS Number
1352066-68-2
Molecular Formula
C28H35Cl2NO5S
Formula Weight
568.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2)(1:2): 0.33 mg/ml
SMILES
O=C1N([C@@H](C(C)C)CS(C(C)C)(=O)=O)[C@H](C2=CC=C(Cl)C=C2)[C@@H](C3=CC(Cl)=CC=C3)C[C@]1(C)CC(O)=O
InChi Code
InChI=1S/C28H35Cl2NO5S/c1-17(2)24(16-37(35,36)18(3)4)31-26(19-9-11-21(29)12-10-19)23(20-7-6-8-22(30)13-20)14-28(5,27(31)34)15-25(32)33/h6-13,17-18,23-24,26H,14-16H2,1-5H3,(H,32,33)/t23-,24-,26-,28-/m1/s1
InChi Key
DRLCSJFKKILATL-YWCVFVGNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $95

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    5 mg

    $279

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    10 mg

    $510

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    Cayman Chemical
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    Product Description

    AMG 232 is an inhibitor of the murine double minute 2 (MDM2) interaction with the tumor suppressor p53 (KD = 0.045 nM; IC50 = 0.6 nM in a cell-free binding assay).1 It inhibits proliferation of HCT116 p53 wild-type, but not p53-/-, cells (IC50s = 10 nM and >25 µM, respectively).2 It reduces tumor growth in an SJSA-1 osteosarcoma mouse xenograft model (ED50 = 9.1 mg/kg) and induces complete regression of tumors in the same model when administered at a dose of 75 mg/kg per day for 10 days.2,1 It induces apoptosis of SJSA-1 mouse xenograft tumor cells, decreasing BrdU-labeled cells, increasing cleaved caspase-3, and halting the cell cycle.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Canon, J., Osgood, T., Olson, S.H., et al. The MDM2 inhibitor AMG 232 demonstrates robust antitumor efficacy and potentiates the activity of p53-inducing cytotoxic agents. Mol. Cancer Ther. 14(3), 649-658 (2015).

    2. Sun, D., Li, Z., Rew, Y., et al. Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development. J. Med. Chem. 57(4), 1454-1472 (2014).