AMG 232

Based on 236 reference(s) in Google Scholar 8 10 236

Axon 2639

CAS [1352066-68-2]

MF C28H35Cl2NO5S
MW 568.55

Purity: 100%
Optical purity: Optically pure
Soluble in 0.1N NaOH(aq) and DMSO

AMG 232

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.

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.

Apoptosis Cell Cycle Regulation Cell Signaling & Oncology Transcription Factors p53-Tumor Suppression DNA-damage Response Ubiquitin EC 6.3.2.19 HDM-MDM

Potent, selective, and orally bioavailable MDM2-p53 inhibitor

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

Parent CAS No.

[1352066-68-2]

产品资料