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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $33 | In Stock | In Stock | |
| 2 mg | $46 | In Stock | In Stock | |
| 5 mg | $72 | In Stock | In Stock | |
| 10 mg | $101 | In Stock | In Stock | |
| 25 mg | $178 | In Stock | In Stock | |
| 50 mg | $286 | In Stock | In Stock | |
| 100 mg | $480 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $78 | In Stock | In Stock |
| 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. |
| Targets&IC50 | JAK1-dependent:36 to 249 nM, JAK:10 to 99 nM |
| 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]. |
| Synonyms | PF-03394197 maleate, PF-03394197 |
| Molecular Weight | 453.51 |
| Formula | C15H23N5O2S·C4H4O4 |
| Cas No. | 1640292-55-2 |
| Smiles | OC(=O)\C=C\C(O)=O.CNS(=O)(=O)C[C@H]1CC[C@@H](CC1)N(C)c1ncnc2[nH]ccc12 |
| Relative Density. | no data available |
| Color | White |
| Appearance | Solid |
| Storage | keep away from direct sunlight,keep away from moisture,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | 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. DMSO: 83 mg/mL (183.02 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.28 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/Ethanol/DMSO
Ethanol/DMSO
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