Oclacitinib CAS NO.1208319-26-9

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) [1]
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) [1].
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 [2].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 [3].