
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)






Size | Price / USD | Stock | Quantity |
2MG | 86 | Get Quote |
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5MG | 132 | Get Quote |
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10MG | 205 | Get Quote |
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25MG | 417 | Get Quote |
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50MG | 615 | Get Quote |
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100MG | 876 | Get Quote |
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200MG | Get Quote | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameAMG 232
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NoteResearch use only, not for human use.
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Brief DescriptionAMG 232 is a potent, selective, orally bioavailable MDM2-p53 inhibitor with Kd of 0.045 nM.
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DescriptionAMG 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.
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In VitroNavtemadlin (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.
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In VivoNavtemadlin (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.
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SynonymsAMG232 | AMG-232
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PathwayApoptosis
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TargetMDM2-p53
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RecptorMDM2-p53
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Research AreaCancer
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IndicationSkin Cancer
Chemical Information
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CAS Number1352066-68-2
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Formula Weight568.5522
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Molecular FormulaC28H35Cl2NO5S
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESCC(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
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Chemical Name3-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
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Storage(-20℃)
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ShippingWith Ice Pack
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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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