Afatinib
Afatinib : ATP-competitive covalent inhibitor of EGFR and ERBB2
Structure
In Cells
In Model Organisms
Probe Afatinib is in the process of SERP review.
Please continue to check back for new reviews and commentary.
SERP ratings and comments
SERP Ratings
SERP Comments:
Potent irreversible inhibitor of EGFR and HER2. Some selectivity data are reported - ideally, a full kinase profile would be required to better understand higher dose range limit. Afatinib hits wild-type;and activating-mutant forms of EGFR with similar potency.
(last updated: 20 May 2016 )
SERP Ratings
SERP Comments:
As a probe for ERBB2 this would not be recommended as it exhibits greater potency for EGFR, more suitable selective probes for ERBB2 exist. Treat the quoted biochemical potency with caution as it is an irreversible inhibitor. Hits WT and activating mutant forms of EGFR with similar potency.
(last updated: 24 May 2016 )