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| | AMG 232 Basic information |
| Product Name: | AMG 232 | | Synonyms: | AMG 232;2-((3R,5R,6S)-5-(3-Chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid;2-[(3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-3-methyl-1-[(2S)-3-methyl-1-propan-2-ylsulfonylbutan-2-yl]-2-oxopiperidin-3-yl]acetic acid(AMG232);CS-1300;AMG-232; AMG 232;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)- | | CAS: | 1352066-68-2 | | MF: | C28H35Cl2NO5S | | MW: | 568.55 | | EINECS: | | | Product Categories: | | | Mol File: | 1352066-68-2.mol |  |
| | AMG 232 Chemical Properties |
| Melting point | 160-164oC | | Boiling point | 732.7±60.0 °C(Predicted) | | density | 1.254±0.06 g/cm3(Predicted) | | storage temp. | -20°C Freezer | | solubility | DMSO (Slightly), Methanol (Slightly) | | pka | 4.29±0.10(Predicted) | | form | Solid | | color | White to Off-White |
| | AMG 232 Usage And Synthesis |
| Uses | AMG-232 is a potent MDM2-P53 inhibitor for use as an anti-tumor agent. | | Biological Activity | amg-232 is a novel inhibitor of p53-mdm2 with ic50 value of 9.2 nm [1].tumor protein p53 (p53) is a very unstable protein with a half-life ranging from 5 to 30 min and participates in a variety of anticancer processes, such as inducing cell apoptosis and inhibiting angiogenesis. mouse double minute 2 homolog (mdm2), also named as e3 ubiquitin-protein ligase mdm2, involves in mediating p53 tumor suppressor. it has been conclusively demonstrated p53 is under-expressed in tumor cells [2].amg-232 is a potent p53-mdm2 interaction inhibitor and is regarded as a promising drug in clinic. when tested with sjsa-1 tumor cell line, amg-232 treatment resulted in cell-cycle arrest and inhibition of tumor cell proliferation via binding to mdm2 protein and robustly inducing p53 activity. it was shown that p53-mdm2 bond rang from a kd of 60 to 700 nm depending on the length of p53 peptide [3].in mouse model with sjsa-1 tumor cells subcutaneous xenograft, co-administration of amg-232 and chemotherapies induced dna damage and p53 activity which resulted in significantly superior antitumor efficacy and regression through arresting cell growth and inducting apoptosis [3]. | | target | MDM2?p53 interaction | | references | [1]. rew, y., et al., discovery of am-7209, a potent and selective 4-amidobenzoic acid inhibitor of the mdm2-p53 interaction. j med chem, 2014. 57(24): p. 10499-511.
[2]. moll, u.m. and o. petrenko, the mdm2-p53 interaction. mol cancer res, 2003. 1(14): p. 1001-8.
[3]. canon, j., et al., the mdm2 inhibitor amg 232 demonstrates robust antitumor efficacy and potentiates the activity of p53-inducing cytotoxic agents. mol cancer ther, 2015. 14(3): p. 649-58. |
| | AMG 232 Preparation Products And Raw materials |
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