LY2874455 is a potent, selective pan-FGFR inhibitor with IC50 of 2.8/2.6/6.4/6 nM for FGFR1/2/3/4, respectively.
LY2874455 inhibits FGFR2 phosphorylation in SNU-16 and KATO-III cells with IC50 of 0.8 and1.5 nM, also inhibits the phosphorylation of FRS2, an immediate downstream target of FGFR, with a similar potency of 0.8 to 1.5 nM.
LY2874455 exhibits a potent activity against FGF/FGFR-mediated signaling in several cancer cell lines and shows an excellent broad spectrum of antitumor activity in several tumor xenograft models representing the major FGF/FGFR relevant tumor histologies including lung, gastric, and bladder cancers and multiple myeloma.
