Lirafugratinib

A covalent FGFR2 inhibitor (IC50 = 0.003 µM), selective for FGFR2 over FGFR1, -3, and -4 (IC50s = 0.77, 0.26, and 15 µM, respectively), inhibits the proliferation of SNU-16 cells (IC50 = 0.002 µM), reduces intratumoral FGFR2 phosphorylation and tumor volume in an FGFR2-amplified SNU-16 gastric cancer mouse xenograft model at 10 mg/kg. Formulation: A solid. InChI: InChI=1S/C28H24FN7O2/c1-15(2)27(37)35-19-8-5-17(6-9-19)24-22(23-25(30)32-14-33-26(23)36(24)4)18-7-10-21(20(29)13-18)38-28-31-12-11-16(3)34-28/h5-14H,1H2,2-4H3,(H,35,37)(H2,30,32,33). InChIKey: XOQVZSSDIQQUGO-UHFFFAOYSA-N. SMILES: O=C(C(C)=C)NC1=CC=C(C2=C(C3=C(N)N=CN=C3N2C)C4=CC(F)=C(OC5=NC=CC(C)=N5)C=C4)C=C1