A-1210477
BH3 mimetic of MCL1
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
SERP Comments:
One might have expected rodent data on A-1210477 to have appeared by now, suggesting the experiments may not have worked. For cell-line studies, some of the less active analogues in PMID 25679114 would be useful specificity controls. Note, covalent probes for the same target have been reported in PMID: 27595327
(last updated: 13 Apr 2017 )
SERP Ratings
SERP Comments:
There are much better probes for MCL-1 now available with significantly better cell potency and demonstrated in vivo efficacy, such as AMG-176 (disclosed in 2017 AACR and ACS; Ki = 50 pM), AZD5991 (disclosed in 2017 AACR; Ki = 130 pM), and S63845 (disclosed in 2016 Nature paper; Ki ~ 1 nM). I would not nominate A-1210477, as the other compounds are substantially better.
(last updated: 17 Apr 2017 )
SERP Ratings
(last updated: 20 Apr 2017 )