MI-77301
Antagonist of MDM2
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
SERP Comments:
MI-77301 (synonym SAR405838) is a highly potent and selective MDM2 inhibitor (Ki=0.88 nM). MI-77301 inhibits the cell growth of cancer cell lines like p53 wild-type osteosarcoma SJSA-1 cell line (IC50=92 nM). The in vivo efficacy of the compound was shown in particular in the SJSA-1 osteosarcoma xenograft model.
(last updated: 8 Aug 2017 )
SERP Ratings
(last updated: 18 Aug 2017 )
SERP Ratings
SERP Comments:
This probe is the result of extensive chemistry optimization over the last 10 years. The original compound was a rationally designed inhibitor of the interaction between p53 and MDM2, but it had liabilities that prevented clinical development. This latest compound appears to be outstanding in both cells and a variety of mouse xenograft cancer models.
(last updated: 18 Aug 2017 )
SERP Ratings
(last updated: 29 Apr 2019 )