Oclacitinib maleate (PF-03394197)

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
100mg	$400	In Stock
250mg	$700	In Stock
500mg	$1050	In Stock

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Cat #: V2550 CAS #: 1640292-55-2 Purity ≥ 98%

Description: 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.

References: 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.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	453.51
Molecular Formula	C15H23N5O2S.C4H4O4
CAS No.	1640292-55-2
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 90 mg/mL (198.5 mM)r
	Water: 18 mg/mL (39.7 mM)r
	Ethanol: 90 mg/mL (198.5 mM)
SMILES Code	O=S(C[C@H]1CC[C@H](N(C)C2=C3C(NC=C3)=NC=N2)CC1)(NC)=O.O=C(O)/C=CC(O)=O
Synonyms	PF 03394197 maleate; Apoquel; PF-03394197 maleate; PF03394197 maleate;

Protocol	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).
Protocol	In Vivo	Scratching bouts at the high dose in the Oclacitinib group are significantly less than in the vehicle-only group (P<0.01).

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.2050 mL	11.0251 mL	22.0502 mL	44.1005 mL
5mM	0.4410 mL	2.2050 mL	4.4100 mL	8.8201 mL
10mM	0.2205 mL	1.1025 mL	2.2050 mL	4.4100 mL
20mM	0.1103 mL	0.5513 mL	1.1025 mL	2.2050 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid 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 master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(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.