Pemigatinib

An FGFR inhibitor (IC50s = 0.4, 0.5, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively); selective for FGFR1, FGFR2, and FGFR3 over FGFR4 and KDR (IC50s = 30 and 70 nM, respectively), as well as over a panel of 56 tyrosine and serine/threonine kinases at 10 µM; reduces phosphorylation of FGFR, ERK1/2, and STAT5 in KG-1a acute myeloid leukemia cells in a concentration-dependent manner; inhibits growth in a panel of cancer cell lines expressing constitutively active FGFR (GI50s = 3-362 nM); reduces tumor growth in KATO III, KG-1, and RT-112 mouse xenograft model at 0.3 mg/kg