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AMG 232
- Navtemadlin
- Optical Purity: Optically pure
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C28H35Cl2NO5S
- MW: 568.55
Description
Potent, selective, and orally bioavailable MDM2-p53 inhibitor (IC50 value 9.1 nM, Kd 0.045 nM), demonstrating remarkable pharmacokinetic properties and in vivo antitumor activity in the SJSA-1 osteosarcoma xenograft model. Moreover, AMG 232 activates p53 pathway activity in vivo, and potentiates the activity of p53-inducing cytotoxic agents.
More Information
| Parent CAS No. | 1352066-68-2 |
|---|---|
| Chemical Name | 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 |
| SMILES | N1([C@H](CS(C(C)C)(=O)=O)C(C)C)[C@H](C2=CC=C(Cl)C=C2)[C@@H](C2=CC=CC(Cl)=C2)C[C@@](CC(O)=O)(C)C1=O |&1:1,12,20,29,r| |
| MFCD | N.A. |
| InChi | 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 |
| InChiKey | DRLCSJFKKILATL-YWCVFVGNSA-N |
| CID | 58573469 |
| Short Description | MDM2 inhibitor |
References
- D Sun et al. Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development. J Med Chem. 2014 Feb 27;57(4):1454-72.
- J Canon et al. The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents. Mol Cancer Ther. 2015 Mar;14(3):649-58.
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