Pacritinib CAS# 937272-79-2 帕西替尼(SB1518)

Pacritinib (SB1518) is an orally bioavailable multikinase inhibitor with selectivity for JAK2 and FLT3. In preclinical enzymatic assays, it inhibited JAK2 with an IC50 of ~23 nM and FLT3 with an IC50 of ~22 nM, showing minimal activity against JAK1 and JAK3. In cell-based studies, pacritinib suppressed STAT3 and STAT5 phosphorylation and inhibited proliferation of JAK2V617F-mutant and FLT3-ITD–driven cell lines (IC50 100–300 nM). In murine models of myelofibrosis and acute myeloid leukemia, oral dosing reduced splenomegaly, normalized cytokine levels, and prolonged survival. Pharmacokinetic profiles indicated good oral bioavailability and sustained plasma exposure, supporting further clinical development.