Oclacitinib
Based on 4 publication(s) in Google Scholar
Oclacitinib is a novel JAK inhibitor. Oclacitinib is most potent at inhibiting JAK1 (IC50=10 nM).
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- 純度: 99.03%
- CAS 番号: 1208319-26-9
- 分子式: C15H23N5O2S
- 分子量:337.44
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Oclacitinib
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生物活性
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JAK1 10 nM (IC50) |
JAK2 18 nM (IC50) |
Tyk2 84 nM (IC50) |
JAK3 99 nM (IC50) |
Using isolated enzyme systems and in vitro human or canine cell models, potency and selectivity of Oclacitinib is determined against JAK family members and cytokines that trigger JAK activation in cells. Inhibitory activity of Oclacitinib against JAK family members is determined in isolated enzyme systems. Oclacitinib inhibits JAK1, JAK2, JAK3, and TYK2 by 50% at concentrations (IC50's) of 10, 18, 99, and 84 nM, respectively. Oclacitinib is most potent against the JAK1 enzyme, showing a 1.8-fold selectivity for JAK1 vs. JAK2 and 9.9-fold selectivity toward JAK1 vs. JAK3. Oclacitinib inhibits JAK family members by 50% at concentrations (IC50's) ranging from 10 to 99 nM and does not inhibit a panel of 38 non-JAK kinases (IC50's > 1000 nM). Oclacitinib also inhibits 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 has minimal effects on cytokines that does not activate the JAK1 enzyme in cells (erythropoietin, granulocyte/macrophage colony-stimulating factor, IL-12, IL-23; IC50's > 1000 nM) [1].Topical treatment with Tofacitinib (0.1%) and Oclacitinib (0.1%) leads to significant reduction of cell migration from mouse ear explants compared with vehicle-treated ears (all P < 0.05). The cell counts of MHC class II positive cells (that is, Langerhans cells) are significantly lower in vehicle-treated compared with each JAK inhibitor–treated epidermis (all P < 0.01) [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1208319-26-9
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性状 Solid
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分子量 337.44
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分子式 C15H23N5O2S
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Color White to off-white
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SMILES
CN([C@H]1CC[C@@H](CC1)CS(NC)(=O)=O)C2=C3C(NC=C3)=NC=N2
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別名
PF-03394197
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Virulence
2024 Dec;15(1):2435372. PMID: 39611624 -
Mol Ther Oncol
Enhancement of radio-sensitivity by inhibition of Janus kinase signaling with oclacitinib in canine tumor cell lines. [Abstract]2025 Feb 3;33(1):200946. PMID: 40051504 -
Dev Comp Immunol
Evolutional conservation of molecular structure and antiviral function of a type I interferon, IFN-kappa, in poultry. [Abstract]2018 Dec:89:44-53. PMID: 30092316 -
溶剤 & 溶解度
DMSO : 5 mg/mL (14.82 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (1.48 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
Recombinant human active kinase domains for JAK1, JAK2, JAK3, and TYK2 are used in isolated enzyme assays using Caliper microfluidics technology to determine potency of Oclacitinib against the JAK family members. Sequence homology to the analogous sequences in the canine JAK enzymes are 98, 98, 100, and 90%, respectively. Invitrogen kinase panel testing is performed to determine potency of Oclacitinib toward 38 different non-JAK kinases using their SelectScreen Kinase Profiling Services. Oclacitinib is evaluated at a concentration of 1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
BALB/cAnN (female, 6 weeks old) are used. The JAK inhibitors (Tofacitinib or Oclacitinib) are administered orally or topically 30 minutes before and 4 hours after toluene-2,4-diisocyanate (TDI) challenge because the absorption of Tofacitinib and Oclacitinib is rapid, with plasma concentrations for both Tofacitinib and Oclacitinib peaking at around 1 hour after oral or intravenous administration. Tofacitinib and Oclacitinib both have a short half-life of 2 and 4 hours after administration, respectively. Each drug is diluted in a 0.5% methylcellulose/0.25% Tween 20 solution for oral administration, and a 7:1 acetone:DMSO solution for topical application to concentrations described subsequently. For each drug, a vehicle-only control group and low- and high-dose groups are set. Oral doses are as follows: Tofacitinib, 10 and 30 mg/kg; and Oclacitinib, 30 and 45 mg/kg. Topically administered doses are 0.1, 0.25, and 0.5% for both chemicals. The oral doses of Tofacitinib and Oclacitinib used in this study are selected.
Dogs[3]
Dogs are randomized to one of two treatment groups (i.e. Oclacitinib or placebo) in a 1:1 ratio. Dogs in the Oclacitinib treatment group are given Oclacitinib maleate caplets orally at a dose of 0.4-0.6 mg/kg twice daily. The scored caplets are provided in three strengths containing 3.6, 5.4 and 16 mg of Oclacitinib. Dogs in the placebo treatment group are given the same number of caplets, identical in appearance to Oclacitinib maleate caplets and containing all of the same excipients except Oclacitinib maleate.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (285 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9635 mL | 14.8174 mL | 29.6349 mL | 74.0872 mL |
| 5 mM | 0.5927 mL | 2.9635 mL | 5.9270 mL | 14.8174 mL | |
| 10 mM | 0.2963 mL | 1.4817 mL | 2.9635 mL | 7.4087 mL |
Oclacitinib 関連分類
HY-13577 関連分類
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