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| 1mg |
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Purity: ≥98%
Oclacitinib maleate (formerly PF-03394197 maleate) is a novel and potent inhibitor of JAK (Janus kinase) family members with IC50 values ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM. Oclacitinib did not inhibit a panel of 38 non-JAK kinases and is the most potent at inhibiting JAK1. Oclacitinib also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation as well as pruritus. Cclacitinib is a targeted therapy that selectively inhibits JAK1-dependent cytokines involved in allergy, inflammation, and pruritus and suggests these are the mechanisms by which oclacitinib effectively controls clinical signs associated with allergic skin disease in dogs.
| ln Vitro |
Oclacitinib's efficacy and selectivity against members of the JAK family and cytokines that cause JAK activation in cells are assessed using isolated enzyme systems and in vitro human or canine cell models. In isolated enzyme systems, oclacitinib's inhibitory action against members of the JAK family is ascertained. JAK1, JAK2, JAK3, and TYK2 are all 50% inhibited by oclacitinib at doses (IC50's) of 10, 18, 99, and 84 nM, respectively. With a 1.8-fold selectivity for JAK1 vs. JAK2 and a 9.9-fold selectivity for JAK1 vs. JAK3, oclacitinib exhibits the highest potency against the JAK1 enzyme. Oclacitinib does not inhibit a panel of 38 non-JAK kinases (IC50's >1000 nM), yet it inhibits JAK family members by 50% at doses (IC50's) ranging from 10 to 99 nM. At IC50 values ranging from 36 to 249 nM, oclacitinib also reduces the activity of JAK1-dependent cytokines implicated in allergy, inflammation, and pruritus (IL-2, IL-4, IL-6, and IL-13). Oclacitinib has negligible effects on cytokines (erythropoietin, granulocyte/macrophage colony-stimulating factor, IL-12, IL-23; IC50's >1000 nM) that do not activate the JAK1 enzyme in cells[1]. Topical treatment with Tofacitinib (0.1%) and Oclacitinib (0.1%) significantly reduces cell migration from mouse ear explants when compared to ears treated with vehicle (all P < 0.05). When compared to each epidermis treated with a JAK inhibitor, the numbers of MHC class II positive cells, or Langerhans cells, are significantly lower in the vehicle-treated epidermis (all P<0.01)[2].
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| ln Vivo |
Scratching bouts at the high dose in the Oclacitinib group are considerably less than in the vehicle-only group (P<0.01)[2]. Client-owned dogs (n=436) with moderate to severe owner-assessed pruritus and a presumptive diagnosis of allergic dermatitis are included. Dogs are randomized to receive Oclacitinib at 0.4-0.6 mg/kg orally twice day or an excipient-matched placebo. An improved 10 cm visual analog scale (VAS) is used to assess the intensity of pruritus from day 0 to 7 and to assess the severity of dermatitis on days 0 and 7. Dogs can remain on the research for 28 days. Oclacitinib produces a rapid onset of effectiveness within 24 h[3].
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| Animal Protocol |
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| References |
[1]. Gonzales AJ, et al. Oclacitinib (APOQUEL) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. J Vet Pharmacol Ther. 2014 Aug;37(4):317-24.
[2]. Fukuyama T, et al. Topically Administered Janus-Kinase Inhibitors Tofacitinib and Oclacitinib Display Impressive Antipruritic and Anti-Inflammatory Responses in a Model of Allergic Dermatitis. J Pharmacol Exp Ther. 2015 Sep;354(3):394-405. [3]. Cosgrove SB, et al. Efficacy and safety of oclacitinib for the control of pruritus and associated skin lesions in dogs with canine allergic dermatitis. Vet Dermatol. 2013 Oct;24(5):479-e114 |
| Molecular Formula |
C15H23N5O2S.C4H4O4
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| Molecular Weight |
453.51
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| CAS # |
1640292-55-2
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| Related CAS # |
Oclacitinib;1208319-26-9
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O=S(C[C@H]1CC[C@H](N(C)C2=C3C(NC=C3)=NC=N2)CC1)(NC)=O.O=C(O)/C=C\C(O)=O
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| Chemical Name |
N-methyl-1-((1r,4r)-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide maleate
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| Synonyms |
PF 03394197 maleate; Apoquel; PF-03394197 maleate; PF03394197 maleate;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2050 mL | 11.0251 mL | 22.0502 mL | |
| 5 mM | 0.4410 mL | 2.2050 mL | 4.4100 mL | |
| 10 mM | 0.2205 mL | 1.1025 mL | 2.2050 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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