Peficitinib

944118-01-8

C18H22N4O2

DMSO : >= 60 mg/mL (183.83 mM)

Epigenetics; Stem Cell/Wnt; JAK/STAT Signaling

Peficitinib is an oral JAK inhibitor, with IC₅₀s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. IC50 & Target: IC50: 3.9 nM (JAK1), 5.0 nM (JAK2), 0.7 nM (JAK3), 4.8 nM (Tyk2)^[1] In Vitro: Peficitinib is an oral JAK inhibitor, with IC₅₀s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. Peficitinib inhibits IL-2-induced T cell proliferation with an IC₅₀ of 10 nM. Peficitinib also suppresses the IL-2-induced STAT5 phosphorylation in rat and human whole blood, with mean IC₅₀s of 124 nM and 127 nM, respectively^[1]. In Vivo: Peficitinib (20 mg/kg, p.o.) suppresses IL-2-induced STAT5 phosphorylation by 78% in the rat model of adjuvant-induced arthritis (AIA). Peficitinib potently inhibits the increase in paw volume (>=1 mg/kg) with an ED₅₀ of 2.7 mg/kg, significantly reduces the bone destruction score (>=10 mg/kg) and almost fully ameliorates both paw swelling and bone destruction scores (30 mg/kg)^[1].