Oclacitinib maleate 是一种新型JAK抑制剂，有效抑制JAK1，IC50为 10 nM。

Oclacitinib is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which did not inhibit a panel of 38 non-JAK kinases.

PF-03394197 inhibits JAK family members by 50% at concentrations ranging from 10 to 99 nM and does not inhibit a panel of 38 non-JAK kinases. PF-03394197 is most potent at inhibiting JAK1. PF-03394197 also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation as well as pruritus. PF-03394197 has minimal effects on cytokines which does not activate the JAK1 enzyme in cells[1].

PF-03394197 administered orally at a dose of 0.4–0.6 mg/kg twice daily is safe and efficacious in controlling the pruritus associated with allergic dermatitis. PF-03394197 provides itch relief within 24 h that persistes through the treatment period, with over 70% of the treated dogs achieving a >50% reduction in pruritus by day 7[2].

1640292-55-2

C19H27N5O6S

453.51

PF-03394197 maleate;奥拉替尼马来酸盐;PF-03394197

Ethanol:83 mg/mL (183 mM)
H2O:15 mg/mL (33.1 mM)
DMSO:83 mg/mL (183 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years