DS-5272 is a potent and orally active p53-MDM2 interaction inhibitor.
Uses
DS-5272 is an orally acitve inhibitor for p53-MDM2 with an IC50 of 20 nM. DS-5272 inhibits the proliferation of SJSA-1 (wildtype p53, IC50=0.17 μM) and DLD-1 (mutant p53). DS-5272 arrest the cell cycle, and induces apoptosis in SJSA-1. DS-5272 exhibits antitumor efficacy in mice[1].
References
[1] Miyazaki M, et al., Discovery of DS-5272 as a promising candidate: A potent and orally active p53-MDM2 interaction inhibitor. Bioorg Med Chem. 2015 May 15;23(10):2360-7. DOI:10.1016/j.bmc.2015.03.069
