CH5183284 is a potent, selective inhibitor of the kinase activity of fibroblast growth factor receptors (FGFRs) 1, 2, and 3 (IC50s = 9.3, 7.6, and 22 nM, respectively). It less potently inhibits FGFR4 and platelet-derived growth factor receptor β (IC50s = 290 and 560 nM, respectively) and displays IC50 values greater than 1 μM for a diverse panel of tyrosine and serine/threonine kinases. CH5183284 is effective against FGFR2 containing the gatekeeper mutation V564F. Moreover, it inhibits the growth of cancer cells expressing FGFR genetic alterations both in vitro and in xenograft mouse models.
