Cat. No.: HY-13577A

Oclacitinib monomaleate

(Synonyms: PF-03394197 monomaleate)

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC₅₀=10 nM).

For research use only. We do not sell to patients.

Purity: 99.87%
CAS No.: 1640292-55-2
Formula: C₁₉H₂₇N₅O₆S
Molecular Weight:453.51

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Oclacitinib monomaleate Chemical Structure

CAS No.: 1640292-55-2

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC₅₀=10 nM).

IC₅₀ & Target^[1]

JAK1

10 nM (IC₅₀)

JAK2

18 nM (IC₅₀)

Tyk2

84 nM (IC₅₀)

JAK3

99 nM (IC₅₀)

All JAK Isoforms :

In Vitro

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.

In Vivo

Scratching bouts at the high dose in the Oclacitinib group are significantly 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 enrolled. Dogs are randomized to either Oclacitinib at 0.4-0.6 mg/kg orally twice daily or an excipient-matched placebo. An enhanced 10 cm visual analog scale (VAS) is used to assess the severity of pruritus from day 0 to 7 and to assess the severity of dermatitis on days 0 and 7. Dogs can remain on the study for 28 days. Oclacitinib produces a rapid onset of efficacy within 24 h^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1640292-55-2
Appearance Solid
Molecular Weight 453.51
Formula C₁₉H₂₇N₅O₆S
Color White to off-white
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
Synonyms

PF-03394197 monomaleate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (4)

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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
Virulence

Blocking virus infection with BacMam virus delivery bovine interferon-α gene. [Abstract]

2024 Dec;15(1):2435372. PMID: 39611624
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
bioRxiv

2025 February 21.

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (551.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 25 mg/mL (55.13 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Protocol

Kinase Assay^[1]

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.

Animal Administration^[2]^[3]

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.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Gonzales AJ, et al. Oclacitinib 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.2050 mL	11.0251 mL	22.0502 mL	55.1256 mL
	5 mM	0.4410 mL	2.2050 mL	4.4100 mL	11.0251 mL
	10 mM	0.2205 mL	1.1025 mL	2.2050 mL	5.5126 mL
	15 mM	0.1470 mL	0.7350 mL	1.4700 mL	3.6750 mL
	20 mM	0.1103 mL	0.5513 mL	1.1025 mL	2.7563 mL
	25 mM	0.0882 mL	0.4410 mL	0.8820 mL	2.2050 mL
	30 mM	0.0735 mL	0.3675 mL	0.7350 mL	1.8375 mL
	40 mM	0.0551 mL	0.2756 mL	0.5513 mL	1.3781 mL
	50 mM	0.0441 mL	0.2205 mL	0.4410 mL	1.1025 mL
DMSO	60 mM	0.0368 mL	0.1838 mL	0.3675 mL	0.9188 mL
	80 mM	0.0276 mL	0.1378 mL	0.2756 mL	0.6891 mL
	100 mM	0.0221 mL	0.1103 mL	0.2205 mL	0.5513 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Oclacitinib monomaleate

4 Cited Publications

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Oclacitinib monomaleate

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Publications Citing Use of MedChemExpress (MCE) Oclacitinib monomaleate

All JAK Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Oclacitinib monomaleate Related Classifications

HY-13577A Related Classifications