PF-06826647

2127109-84-4

383.41

DMSO : 16.67 mg/mL (43.48 mM; Need ultrasonic)

Epigenetics; Stem Cell/Wnt; JAK/STAT Signaling

PF-06826647 is an orally active and selective TYK2 inhibitor (IC₅₀=17 nM), which binds to TYK2 catalytically active JH1 domain. PF-06826647 displays selectivity for TYK2 over JAK1 (IC₅₀=383 nM) and JAK2 (74 nM). PF-06826647 can be used for the research of psoriasis, ulcerative colitis, and hidradenitis suppurativa^[1][2]. IC50 & Target: IC50: 17 nM (TYK2 JH1)^[1] In Vitro: PF-06826647 inhibits a panel of 231 kinases at non-physiologically conditions for each kinase Km showed 21 non-JAK kinases with >50% at 1 uM dose^[2]. In Vivo: PF-06826647 (30, 10, 3 mg/kg, p.o.; once per day) reduces clinical end points associated with the mouse imiquimod-induced skin inflammation model. The measured average unbound daily concentrations of 1, 3, 10, and 30 mg/kg are 14.5, 45.7, 225, and 668 nM, respectively, resulting in average IL-12 inhibition of 51, 77, 94, and 98%^[2].
PF-06826647 (1 mg/kg; i.v.; sprague-Dawley rats) shows the systemic clearance is 12 (mL/min)/kg, the steady state volume of distribution (V_ss) is 1.1 L/kg, and the AUC_inf is 1380 ng-h/ mL^[2].