Pemigatinib CAS# 1513857-77-6 培米加替尼

Pemigatinib (INCB054828) is a potent, ATP-competitive inhibitor of FGFR1–3, with IC₅₀ values of approximately 0.4, 0.4, and 1 nM, respectively, and minimal activity against FGFR4 (IC₅₀ ~30 nM). In vitro, it strongly suppresses FGFR phosphorylation and downstream signaling (p‑ERK and p‑STAT5) at concentrations as low as 5 nM, selectively impairing growth of cancer cell lines harboring FGFR alterations. When orally administered at doses beginning around 0.3 mg/kg, pemigatinib significantly inhibited tumor growth in xenograft models of AML (FGFR1-driven), cholangiocarcinoma (FGFR2-driven), and urothelial carcinoma (FGFR3-driven).