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Oclacitinib maleate

🥰Excellent
Catalog No. T6914Cas No. 1640292-55-2
Alias PF-03394197 maleate, PF-03394197

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.

Oclacitinib maleate

Oclacitinib maleate

🥰Excellent
Purity: 99.92%
Catalog No. T6914Alias PF-03394197 maleate, PF-03394197Cas No. 1640292-55-2
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$33In StockIn Stock
2 mg$46In StockIn Stock
5 mg$72In StockIn Stock
10 mg$101In StockIn Stock
25 mg$178In StockIn Stock
50 mg$286In StockIn Stock
100 mg$480In StockIn Stock
1 mL x 10 mM (in DMSO)$78In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.92%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
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
JAK:10 to 99 nM, JAK1-dependent:36 to 249 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].
SynonymsPF-03394197 maleate, PF-03394197
Chemical Properties
Molecular Weight453.51
FormulaC15H23N5O2S·C4H4O4
Cas No.1640292-55-2
SmilesOC(=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
Storage & Solubility Information
Storagekeep 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 recommended.
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
1mg5mg10mg50mg
1 mM2.2050 mL11.0251 mL22.0502 mL110.2512 mL
5 mM0.4410 mL2.2050 mL4.4100 mL22.0502 mL
10 mM0.2205 mL1.1025 mL2.2050 mL11.0251 mL
20 mM0.1103 mL0.5513 mL1.1025 mL5.5126 mL
Ethanol/DMSO
1mg5mg10mg50mg
50 mM0.0441 mL0.2205 mL0.4410 mL2.2050 mL
100 mM0.0221 mL0.1103 mL0.2205 mL1.1025 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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