FIIN-1 (FGFR irreversible inhibitor-1) is an irreversible and selective FGFR inhibitor with Kd of 2.8, 6.9, 5.4, 120, 32 and 120 nM for FGFR1, FGFR2, FGFR3, FGFR4, Flt1, Flt14, respectively.FIIN-1 inhibited FGFR1, FGFR2, FGFR3, FGFR4, with IC50 of 9.2, 6.2, 11.9 and 189 nM. FIIN-1 inhibited FGFR1, FGFR2, FGFR3 and FGFR4, with IC50s of 9.2, 6.2, 11.9 and 189 nM, respectively.

FGFR2:6.9 nM (Kd), FGFR2:6.2 nM (IC50), FGFR1:9.2 nM (IC50), FGFR1:2.8 nM (Kd), FGFR3:5.4 nM (Kd), FGFR3:11.9 nM (IC50), FGFR4:189 nM (IC50), FGFR4:120 nM (Kd)

FIIN-1 (14 nM-46 μM; 72 h; ) inhibits the proliferation of FGF signaling-sensitive cancer cell lines. The EC50s of 70 nM, 230 nM, 2.3 μM, for Bladder RT4, Pancreas A2.1, Bone RD-ES cells. EC50s of 0.22 and 4.6 μM for Ovary A2780 and PA-1 cells, respectively. EC50s of 0.08 and 4.5 μM for Lung SBC-3 and H520 cells, respectively. EC50s of 0.14 and 1.65 μM for Kidney G-401 and G-402 cells, respectively. EC50s of 0.014, 0.03, and 0.65 μM for Stomach KATO III, SNU-16, and FU97 cells, respectively.[1]
FIIN-1 (20 nM) inhibits iFGFR1 autophosphorylation and its downstream Erk1/2 almost completely.[1]
FIIN-1 binds to BLK, ERK5, KIT, MET, PDGFRB, and VEGFR2 with Kds of 65 nM, 160, 420, 1000, 480, and 210 nM, respectively. The IC50s for Blk and Flt1 are 381 nM and 661 nM respectively.[1]