BGJ-398
Inhibitor of FGFR1, FGFR2, FGFR3, FGFR4
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
SERP Comments:
This probe is a potent and selective inhibitor of FGFR1/2/3 (though less potent against FGFR4). It acts as an adequate in vitro and in vivo inhibitor tool for these kinases.
(last updated: 23 May 2016 )
SERP Ratings
SERP Comments:
This compound is a pan FGFR inhibitor in the nM range with other kinases only being inhibited at high (triple digit) nM or low uM in cells. I think this probe is the best so far though, ideally, there would be separate probes for FGFR 1-4.
(last updated: 1 Jun 2016 )
SERP Ratings
SERP Comments:
This probe has single-digit nM potency on FGFR1,2,3 in both in vitro biochemical and cell-based assays. It shows potency against only 76 other kinases assayed with most significant activity on FGFR4 (60 nM) and VEGFR2 (180 nM). Its selectivity against several related kinases remains unknown, however, (e.g. FLT1, CSFR, c-Kit, etc), which leads to some concern. Control of FGFR-driven tumor xenograft seen at doses 5 mg/kg - 30 mg/kg in multiple models. The preferred probe for FGFR4 is BLU9931 (Cancer Discovery, Hagel et al. 2015).
(last updated: 7 Jun 2016 )