Imatinib
ATP-competitive inhibitor of ABL1, KIT
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
SERP Comments:
This compound has inadequate selectivity to be considered a probe.
(last updated: 24 May 2016 )
SERP Ratings
SERP Comments:
Imatinib is a non-selective kinase inhibitor originally developed as a tyrosine kinase inhibitor, as shown in several papers (Nature Biotechnology 23, 329 - 336 (2005) ; Nature Biotechnology 26, 127 - 132 (2008) ). Imatinib is a potent inhibitior of ABL (Kis in the 10s of nM), DDR1 (Ki=0.8 nM), DDR2 (Ki=15 nM), KIT (Ki=14 nM), LCK (K=40 nM), PDGFRB (Ki=14 nM), PDGFRA (Ki=30 nM) and has affinity for many other kinases (see http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?tab=screens&ligandId=5687). Imatinib also has high affinity for the human quinone reductase 2 (NQO2) (Ki=80 nM; BMC Struct Biol. 2009; 9: 7).
(last updated: 6 Jun 2016 )
SERP Ratings
(last updated: 16 Mar 2017 )
Portal Comments
In a 2023 study, Hu et al. evaluated Imatinib in live-cell assays for Phospholipidosis induction, cautioning about adverse effects at concentrations equal or exceeding 1 uM. (DOI: 10.1016/j.chembiol.2023.09.003)
(last updated: 7 Nov 2023)