MedKoo Cat#: 574826 | Name: Oclacitinib maleate
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Oclacitinib, also known as PF03394197, is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. Oclacitinib inhibited JAK family members by 50% at concentrations (IC50 's) ranging from 10 to 99 nM and did not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nm). Oclacitinib was most potent at inhibiting JAK1 (IC50 = 10 nm). Oclacitinib also inhibited 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.

Chemical Structure

Oclacitinib maleate
Oclacitinib maleate
CAS#1208319-27-0 (maleate)

Theoretical Analysis

MedKoo Cat#: 574826

Name: Oclacitinib maleate

CAS#: 1208319-27-0 (maleate)

Chemical Formula: C19H27N5O6S

Exact Mass: 453.1682

Molecular Weight: 453.51

Elemental Analysis: C, 50.32; H, 6.00; N, 15.44; O, 21.17; S, 7.07

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,450.00 2 Weeks
1g USD 3,850.00 2 Weeks
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Synonym
Oclacitinib maleate; PF-03394197 maleate; PF-03394197-11; PF03394197-11; PF 03394197-11;
IUPAC/Chemical Name
N-methyl-1-((1r,4r)-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide maleate
InChi Key
VQIGDTLRBSNOBV-VQIYXBGXSA-N
InChi Code
InChI=1S/C15H23N5O2S.C4H4O4/c1-16-23(21,22)9-11-3-5-12(6-4-11)20(2)15-13-7-8-17-14(13)18-10-19-15;5-3(6)1-2-4(7)8/h7-8,10-12,16H,3-6,9H2,1-2H3,(H,17,18,19);1-2H,(H,5,6)(H,7,8)/b;2-1-/t11-,12-;
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=C\C(O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Biological target:
Oclacitinib, also known as PF03394197, is a novel Janus kinase inhibitor.
In vitro activity:
The results indicate that beneficial effects of OCL in the treatment of skin allergic diseases may be partially mediated by the inhibition of IL-4 production in CD4+ and CD8+ T cells. To a certain extent, the antiproliferative effect of OCL on CD8+ T cells may also contribute to its therapeutic effect. Moreover, OCL was found to counteract the induction of type 1 regulatory T (Tr1) cells and to act as a strong inhibitor of IL-10 production in both CD4+ and CD8+ T cells. Reference: Molecules. 2021 Sep 17;26(18):5655. https://pubmed.ncbi.nlm.nih.gov/34577127/
In vivo activity:
The primary objective of this study was to mimic the rebound phenomenon of oclacitinib using a chronic pruritic mouse model of allergic contact dermatitis. Mice treated with oclacitinib showed a significant decrease in scratching bouts during treatment, then following abrupt withdrawal scratching bouts were significantly increased. Furthermore, following abrupt withdrawal more DRG neurons were activated by pruritogenic cytokines, TNFα positive DCs were significantly increased, and affected skin revealed a significant increase of TNFα and TSLP. Reference: Eur J Pharmacol. 2017 Jan 5;794:20-26. https://pubmed.ncbi.nlm.nih.gov/27847179/

Preparing Stock Solutions

The following data is based on the product molecular weight 453.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Jasiecka-Mikołajczyk A, Jaroszewski JJ, Maślanka T. Oclacitinib, a Janus Kinase Inhibitor, Reduces the Frequency of IL-4- and IL-10-, but Not IFN-γ-, Producing Murine CD4+ and CD8+ T Cells and Counteracts the Induction of Type 1 Regulatory T Cells. Molecules. 2021 Sep 17;26(18):5655. doi: 10.3390/molecules26185655. PMID: 34577127; PMCID: PMC8472008. 2. Gonzales AJ, Bowman JW, Fici GJ, Zhang M, Mann DW, Mitton-Fry M. 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. doi: 10.1111/jvp.12101. Epub 2014 Feb 5. PMID: 24495176; PMCID: PMC4265276. 3. Fukuyama T, Ganchingco JR, Bäumer W. Demonstration of rebound phenomenon following abrupt withdrawal of the JAK1 inhibitor oclacitinib. Eur J Pharmacol. 2017 Jan 5;794:20-26. doi: 10.1016/j.ejphar.2016.11.020. Epub 2016 Nov 12. PMID: 27847179.
In vitro protocol:
1. Jasiecka-Mikołajczyk A, Jaroszewski JJ, Maślanka T. Oclacitinib, a Janus Kinase Inhibitor, Reduces the Frequency of IL-4- and IL-10-, but Not IFN-γ-, Producing Murine CD4+ and CD8+ T Cells and Counteracts the Induction of Type 1 Regulatory T Cells. Molecules. 2021 Sep 17;26(18):5655. doi: 10.3390/molecules26185655. PMID: 34577127; PMCID: PMC8472008. 2. Gonzales AJ, Bowman JW, Fici GJ, Zhang M, Mann DW, Mitton-Fry M. 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. doi: 10.1111/jvp.12101. Epub 2014 Feb 5. PMID: 24495176; PMCID: PMC4265276.
In vivo protocol:
1. Fukuyama T, Ganchingco JR, Bäumer W. Demonstration of rebound phenomenon following abrupt withdrawal of the JAK1 inhibitor oclacitinib. Eur J Pharmacol. 2017 Jan 5;794:20-26. doi: 10.1016/j.ejphar.2016.11.020. Epub 2016 Nov 12. PMID: 27847179.
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.