| Name | Oclacitinib maleate |
| Description | Oclacitinib maleate (PF-03394197 maleate) is a novel inhibitor of JAK family members, with IC50 values ranging from 10 to 99 nM, and JAK1-dependent cytokines, with IC50 ranging from 36 to 249 nM, while not inhibiting a panel of 38 non-JAK kinases. |
| In vitro | Oclacitinib 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. Oclacitinib is most potent at inhibiting JAK1. Oclacitinib also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation as well as pruritus. Oclacitinib has minimal effects on cytokines which does not activate the JAK1 enzyme in cells[1]. |
| In vivo | Oclacitinib 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. Oclacitinib 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 15 mg/mL (33.08 mM), Sonication is recommended.
Ethanol : 83 mg/mL (183.02 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (7.28 mM), Sonication is recommended.
DMSO : 83 mg/mL (183.02 mM), Sonication is recommended.
|
| Keywords | TyrosineKinases | Tyrosine Kinases | TYK2 | PF-03394197 Maleate | PF03394197 Maleate | PF03394197 | PF 03394197 Maleate | PF 03394197 | Oclacitinib maleate | Oclacitinib | Janus kinase | JAK3 | JAK2 | JAK1-dependent | JAK1 | JAK | Inhibitor | inhibit |
| Inhibitors Related | Alectinib | Ruxolitinib | Atinvicitinib | Tofacitinib Citrate | Resveratrol | Soquelitinib | Ibrutinib | Vidarabine | JAK-IN-10 | 2,4,5-Trimethoxybenzoic acid | Gefitinib | Lentinan |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Kinase Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
