Oclacitinib maleate — Datasheet

Biological Activity

Oclacitinib(PF03394197) is a potent and selective JAKs inhibitor with IC50 of 10-99 nM; not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nM). IC50 value: 10 nM (JAK1) Target: JAKs in vitro: Oclacitinib inhibited the function of JAK1-dependent cytokines involved in allergy and inflammation (IL-2, IL-4, IL-6, and IL-13) as well as pruritus (IL-31) at IC50 's ranging from 36 to 249 nm. Oclacitinib had minimal effects on cytokines that did not activate the JAK1 enzyme in cells (erythropoietin, granulocyte/macrophage colony-stimulating factor, IL-12, IL-23; IC50 's > 1000 nm) . in vivo: Dogs were randomized to receive either oclacitinib (0.4-0.6 mg/kg twice daily for 14 days and then once daily for up to 112 days) or an excipient-matched placebo .Dogs were randomized to either oclacitinib at 0.4-0.6 mg/kg orally twice daily or an excipient-matched placebo. An enhanced 10 cm visual analog scale (VAS) was used by the owners to assess the severity of pruritus from day 0 to 7 and by veterinarians to assess the severity of dermatitis on days 0 and 7. Dogs could remain on the study for 28 days . For the detailed information of PF-03394197, the solubility of PF-03394197 in water, the solubility of PF-03394197 in DMSO, the solubility of PF-03394197 in PBS buffer, the animal experiment (test) of PF-03394197, the cell expriment (test) of PF-03394197, the in vivo, in vitro and clinical trial test of PF-03394197, the EC50, IC50,and Affinity of PF-03394197, Please contact DC Chemicals.

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.