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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Oclacitinib (formerly also known as PF-03394197) 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 |
Potency and selectivity of oclacitinib 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. Oclacitinib's inhibitory activity against members of the JAK family is assessed using isolated enzyme systems; at concentrations (IC50's) of 10, 18, 99, and 84 nM, respectively, oclacitinib inhibits JAK1, JAK2, JAK3, and TYK2 by 50%. 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 comparing each epidermis treated with a JAK inhibitor to that treated with a vehicle, the numbers of MHC class II positive cells, or Langerhans cells, are significantly reduced (all P < 0.01) [2].
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| ln Vivo |
There are considerably fewer scratching episodes at the high dose in the Oclacitinib group (P<0.01) compared to the vehicle-only group. Enrollment of client-owned dogs (n = 436) with a probable diagnosis of allergic dermatitis and moderate to severe owner-assessed pruritus occurs. Dogs are randomized to receive an excipient-matched placebo or oclacitinib at a dose of 0.4–0.6 mg/kg orally twice a day. The intensity of dermatitis is measured on days 0 and 7, and the degree of pruritus is measured from day 0 to day 7 using an improved 10 cm visual analog scale (VAS). Dogs can spend up to 28 days in the trial. Oclacitinib has a 24-hour quick onset of action[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
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| Molecular Weight |
337.44
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| CAS # |
1208319-26-9
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| Related CAS # |
Oclacitinib maleate;1640292-55-2;Oclacitinib-13C-d3
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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
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| Synonyms |
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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 |
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| 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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9635 mL | 14.8174 mL | 29.6349 mL | |
| 5 mM | 0.5927 mL | 2.9635 mL | 5.9270 mL | |
| 10 mM | 0.2963 mL | 1.4817 mL | 2.9635 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.
Vet Dermatol.2013 Oct;24(5):479-e114. |
Vet Dermatol.2013 Oct;24(5):479-e114. |
Vet Dermatol.2013 Oct;24(5):479-e114. |
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