A-770041
Inhibitor of LCK
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
SERP Comments:
This is a selective probe within the src family of RTK’s as described. Selectivity outside this family has been mentioned, but data not provided. From JPET paper: “A-770041 is 60-fold selective against Src, 95-fold selective against Fgr, and 300-fold selective against Fyn. A-770041 was also greater than 200-fold selective against a secondary battery of approximately 20 serine/threonine and tyrosine kinases outside of the Src family and IC50 values greater than 10 uM in a CEREP panel of approximately 70 molecular targets (data not shown).”
(last updated: 18 Dec 2020 )
SERP Ratings
SERP Comments:
Initial studies involving development and medicinal chemistry were performed against purified proteins (including selectivity panels) and in vivo in rats and mice. Two later studies used this probe in cells to potentiate chemotherapies, in which case a range of concentrations were tested, and to target an acute myeloid leukemia cell line known to have a mutant dysregulated Lck protein. The latter studies provide good evidence for cellular engagement of the target in a selective way.
(last updated: 19 Jan 2021 )
SERP Ratings
(last updated: 29 Mar 2021 )