AMG 232

CAS No. 1352066-68-2

AMG 232( AMG232 | AMG-232 )

Catalog No. M11426 CAS No. 1352066-68-2

AMG 232 is a potent, selective, orally bioavailable MDM2-p53 inhibitor with Kd of 0.045 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 86 Get Quote
5MG 132 Get Quote
10MG 205 Get Quote
25MG 417 Get Quote
50MG 615 Get Quote
100MG 876 Get Quote
200MG Get Quote Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    AMG 232
  • Note
    Research use only, not for human use.
  • Brief Description
    AMG 232 is a potent, selective, orally bioavailable MDM2-p53 inhibitor with Kd of 0.045 nM.
  • Description
    AMG 232 is a potent, selective, orally bioavailable MDM2-p53 inhibitor with Kd of 0.045 nM, inhibits SJSA-1 cell proliferation with IC50 of 9.1 nM; robustly induces p53 activity, leading to cell-cycle arrest and inhibition of tumor cell proliferation; significantly inhibits tumor growth in SJSA-1 osteosarcoma xenograft model with ED50 of 9.1 mg/kg, also showsignificantly superior antitumor efficacy chombined with chemotherapies in vivo, enhances radiosensitivity via inhibition of damage repair signaling.Skin Cancer Phase 2 Clinical.
  • In Vitro
    Navtemadlin (AMG 232) (10 μM) induces p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines. Navtemadlin potently inhibits proliferation of non-MDM2-amplified HCT116 colorectal cells (IC50=10 nM).Cell Viability AssayCell 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
    Navtemadlin (AMG 232) (10, 25, 75 mg/kg, once daily, p.o.) activates p53 pathway activity in vivo.Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) potently inhibits growth of tumor xenografts in mice.Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) blocks DNA synthesis and induces apoptosis in vivo.Navtemadlin causes a dose-dependent tumor growth inhibition with an ED50 of 16 mg/kg. Animal Model:Female athymic nude mice (n=10/group) based cancer models.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.
  • Synonyms
    AMG232 | AMG-232
  • Pathway
    Apoptosis
  • Target
    MDM2-p53
  • Recptor
    MDM2-p53
  • Research Area
    Cancer
  • Indication
    Skin Cancer

Chemical Information

  • CAS Number
    1352066-68-2
  • Formula Weight
    568.5522
  • Molecular Formula
    C28H35Cl2NO5S
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    CC(C)S(C[C@H](C(C)C)N(C1=O)[C@@H]([C@H](C[C@@]1(CC(O)=O)C)C2=CC=CC(Cl)=C2)C3=CC=C(C=C3)Cl)(=O)=O
  • Chemical Name
    3-Piperidineacetic acid, 5-(3-chlorophenyl)-6-(4-chlorophenyl)-3-methyl-1-[(1S)-2-methyl-1-[[(1-methylethyl)sulfonyl]methyl]propyl]-2-oxo-, (3R,5R,6S)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Sun D, et al. J Med Chem. 2014 Feb 27;57(4):1454-72. 2. Canon J, et al. Mol Cancer Ther. 2015 Mar;14(3):649-58. 3. Werner LR, et al. Mol Cancer Ther. 2015 Sep;14(9):1994-2003. 4. Prabakaran PJ, et al. Clin Cancer Res. 2017 Oct 15;23(20):6044-6053.
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