Oclacitinib | PF-03394197 | CAS#1208319-26-9 | JAK inhibitor

MedKoo Cat#: 510286 | Name: Oclacitinib

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

CAS#1208319-26-9 (free base)

Theoretical Analysis

MedKoo Cat#: 510286

Name: Oclacitinib

CAS#: 1208319-26-9 (free base)

Chemical Formula: C15H23N5O2S

Exact Mass: 337.1573

Molecular Weight: 337.44

Elemental Analysis: C, 53.39; H, 6.87; N, 20.75; O, 9.48; S, 9.50

Price and Availability

Size	Price	Availability
25mg	USD 150.00	Ready to ship
50mg	USD 250.00	Ready to ship
100mg	USD 400.00	Ready to ship
250mg	USD 650.00	Ready to ship
500mg	USD 950.00	Ready to ship
1g	USD 1,450.00	Ready to ship
2g	USD 2,450.00	Ready to ship

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Related CAS #

1208319-27-0 (maleate) 1640292-55-2 1208319-26-9 (free base)

Synonym

PF03394197; PF-03394197; PF 03394197; Oclacitinib; Apoquel;

IUPAC/Chemical Name

N-methyl-1-((1r,4r)-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide

InChi Key

HJWLJNBZVZDLAQ-HAQNSBGRSA-N

InChi Code

InChI=1S/C15H23N5O2S/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/h7-8,10-12,16H,3-6,9H2,1-2H3,(H,17,18,19)/t11-,12-

SMILES Code

O=S(C[C@H]1CC[C@H](N(C)C2=C3C(NC=C3)=NC=N2)CC1)(NC)=O

Appearance

white to off-white 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, not in water

Shelf Life

>2 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

Product Data

Certificate of Analysis

View CoA: current batch, lot#TZC41222

QC Data

View QC data, current batch, lot#TZC41222

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

Oclacitinib, also known as PF03394197, is a JAK family inhibitor by 50% at concentrations (IC50 's) ranging from 10 to 99 nM and has activity against cytokines involved in allergy.

In vitro activity:

The objective of this study was to determine whether the novel JAK inhibitor oclacitinib could reduce the activity of cytokines implicated in canine allergic skin disease. Using isolated enzyme systems and in vitro human or canine cell models, potency and selectivity of oclacitinib was determined against JAK family members and cytokines that trigger JAK activation in cells. 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. Oclacitinib had minimal effects on cytokines that did not activate the JAK1 enzyme in cells (erythropoietin, granulocyte/macrophage colony-stimulating factor, IL-12, IL-23; IC50's > 1000 nm). These results demonstrate that oclacitinib is a targeted therapy that selectively inhibits JAK1-dependent cytokines involved in allergy, inflammation, and pruritus and suggests these are the mechanisms by which oclacitinib effectively controls clinical signs associated with allergic skin disease in dogs. J Vet Pharmacol Ther. 2014 Aug; 37(4): 317–324. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4265276/

In vivo activity:

The aim of this study was to evaluate the safety and clinical effects of oral oclacitinib maleate in healthy cats. Thirty mixed-breed cats weighing from 2.1 to 5.3 kg each were randomly allocated to three treatment groups of 10 animals each. Cats in two groups received oclacitinib at 1 mg/kg or 2 mg/kg q 12 h orally for 28 days. Cats in the third group were given placebo tablets (cornstarch) q 12 h orally for 28 days. There were no significant differences in white blood cell counts between groups at any sampling time. Neutrophil mean values also were within the reference range, but there was a transient significant increase on day 21 (p = 0.007) for both treated groups compared with the placebo group. Also on day 21, mean monocyte counts were significantly higher in 1 mg/kg group than in the placebo group (p = 0.03) and significantly lower in 2 mg/kg (p = 0.03); however, values were within the normal reference range. The mean lymphocyte count was within the normal reference range at all samplings for cats in all groups, with no significant differences between placebo and treated cats. A decrease in the mean eosinophil count was observed in both oclacitinib groups, and this decrease was significant between the placebo and treated groups on day 14 (p = 0.04), but the mean value remained within the normal reference range for all days.Oclacitinib was well tolerated by cats at 1 mg/kg and 2 mg/kg and appeared to be a safe medication for this species to be treated twice daily for up to 28 days. BMC Vet Res. 2019; 15: 137. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6506962/

	Solvent	mg/mL	mM
Solubility
	DMSO	12.0	35.60

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 337.44 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.

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. 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. 2. Fukuyama T, Ehling S, Cook E, Bäumer W. 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. doi: 10.1124/jpet.115.223784. Epub 2015 Jul 9. PMID: 26159873. 3. Lopes NL, Campos DR, Machado MA, Alves MSR, de Souza MSG, da Veiga CCP, Merlo A, Scott FB, Fernandes JI. A blinded, randomized, placebo-controlled trial of the safety of oclacitinib in cats. BMC Vet Res. 2019 May 8;15(1):137. doi: 10.1186/s12917019-1893-x. PMID: 31068210; PMCID: PMC6506962. 4. Cosgrove SB, Wren JA, Cleaver DM, Martin DD, Walsh KF, Harfst JA, Follis SL, King VL, Boucher JF, Stegemann MR. 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. doi: 10.1111/vde.12047. Epub 2013 Jul 5. PMID: 23829933; PMCID: PMC4282347.

In vitro protocol:

In vivo protocol:

1. Lopes NL, Campos DR, Machado MA, Alves MSR, de Souza MSG, da Veiga CCP, Merlo A, Scott FB, Fernandes JI. A blinded, randomized, placebo-controlled trial of the safety of oclacitinib in cats. BMC Vet Res. 2019 May 8;15(1):137. doi: 10.1186/s12917019-1893-x. PMID: 31068210; PMCID: PMC6506962. 2. Cosgrove SB, Wren JA, Cleaver DM, Martin DD, Walsh KF, Harfst JA, Follis SL, King VL, Boucher JF, Stegemann MR. 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. doi: 10.1111/vde.12047. Epub 2013 Jul 5. PMID: 23829933; PMCID: PMC4282347.

1: Xu G, You Z, Zheng Y, Feng Q, Luo S, Xu L, Bao S, Wang Q. Integrated microbiome and metabolome analysis reveals that new insight into Radix pseudostellariae polysaccharide enhances PRRSV inactivated vaccine. Front Immunol. 2024 Jun 26;15:1352018. doi: 10.3389/fimmu.2024.1352018. PMID: 38989282; PMCID: PMC11233517. 2: Gonzales AJ, Aleo M, Mahabir S, Messamore J, Stegemann M. Oclacitinib (APOQUEL®) is a selective Janus kinase 1 inhibitor with efficacy in a canine model of flea allergic dermatitis. J Vet Pharmacol Ther. 2024 Jun 26. doi: 10.1111/jvp.13462. Epub ahead of print. PMID: 38926932. 3: Chan T, Koch SN, Devine S, Mendoza-Kuznetsova E. Oclacitinib therapy in two cats with refractory proliferative and necrotising otitis externa. Vet Dermatol. 2024 May 31. doi: 10.1111/vde.13269. Epub ahead of print. PMID: 38818665. 4: C Bergeron C, Costa MC, Segura M, de Souza LB, Bleuzé M, Sauvé F. Bacterial microbiota and proinflammatory cytokines in the anal sacs of treated and untreated atopic dogs: Comparison with a healthy control group. PLoS One. 2024 May 30;19(5):e0298361. doi: 10.1371/journal.pone.0298361. PMID: 38814946; PMCID: PMC11139270. 5: Tham HL, Davis JL. Pharmacology of drugs used in autoimmune dermatopathies in cats and dogs: A narrative review. Vet Dermatol. 2024 Aug;35(4):453-476. doi: 10.1111/vde.13253. Epub 2024 May 6. PMID: 38708551. 6: Wright A, Hillier A, Lambert J, Mwacalimba K, Lloyd N, Kagiwada T, Hashiguchi Y, Hours C, Riley D, Enstone A, Wyn R. Dog Owners' Perceptions of the Convenience and Value of Chewable Oclacitinib: Quantitative Survey Data from an International Survey. Animals (Basel). 2024 Mar 19;14(6):952. doi: 10.3390/ani14060952. PMID: 38540050; PMCID: PMC10967547. 7: Qin JJ, Zhu H, Song ZW, Hou XJ, Wang XM, Wang L, Li JX. A randomized double- blind clinical trial: Comparison of oclacitinib with a traditional Chinese herbal medicine product (Dihuang Guiqin capsule) in the treatment of canine atopic dermatitis. Res Vet Sci. 2024 May;171:105221. doi: 10.1016/j.rvsc.2024.105221. Epub 2024 Mar 11. PMID: 38490043. 8: Yu Y, Chen S, Zhang H, Duan Y, Li Z, Jiang L, Cao W, Peng Q, Chen X. A panel of janus kinase inhibitors identified with anti-inflammatory effects protect mice from lethal influenza virus infection. Antimicrob Agents Chemother. 2024 Apr 3;68(4):e0135023. doi: 10.1128/aac.01350-23. Epub 2024 Mar 12. PMID: 38470034; PMCID: PMC10989010. 9: Schäfer L, Thom N. A placebo-controlled, double-blind study evaluating the effect of orally administered polyunsaturated fatty acids on the oclacitinib dose for atopic dogs. Vet Dermatol. 2024 Aug;35(4):408-417. doi: 10.1111/vde.13246. Epub 2024 Mar 11. PMID: 38465482. 10: Congiusta MC, Snyder C, Soukup JW, Apostolopoulos N. Novel Management of Masticatory Myositis in Three Dogs with a Selective Janus Kinase (JAK-1) Inhibitor. J Vet Dent. 2024 Jan 8:8987564231219925. doi: 10.1177/08987564231219925. Epub ahead of print. PMID: 38192103. 11: Parvathy K. Resolution of hypoalbuminemia in a 3-year-old hound-mix dog after discontinuation of oclacitinib. J Am Vet Med Assoc. 2023 Dec 8;262(3):1-3. doi: 10.2460/javma.23.10.0600. PMID: 38064895. 12: Pérez-Aranda M, Yotti C, Pérez J, Ginel PJ. Successful treatment of sebaceous adenitis with oclacitinib and low-dose prednisolone in a dog. Vet Dermatol. 2024 Apr;35(2):238-241. doi: 10.1111/vde.13216. Epub 2023 Nov 15. PMID: 37968244. 13: Thomsen M, Künstner A, Wohlers I, Olbrich M, Lenfers T, Osumi T, Shimazaki Y, Nishifuji K, Ibrahim SM, Watson A, Busch H, Hirose M. A comprehensive analysis of gut and skin microbiota in canine atopic dermatitis in Shiba Inu dogs. Microbiome. 2023 Oct 21;11(1):232. doi: 10.1186/s40168-023-01671-2. PMID: 37864204; PMCID: PMC10590023. 14: Yuki M, Taira H, Narita M, Inden T, Yokota S, Naito E, Maeda S. Complete remission of two canine cases with precursor-targeted immune-mediated anemia after combination therapy with prednisolone, cyclosporine, and oclacitinib. Open Vet J. 2023 Sep;13(9):1205-1211. doi: 10.5455/OVJ.2023.v13.i9.16. Epub 2023 Sep 30. PMID: 37842117; PMCID: PMC10576580. 15: Baretta LT, do Espírito Santo Cunha V, Figueiredo CD, Gerardi DG. A randomised, double-blinded trial to assess the effect of oclacitinib and prednisolone on intradermal allergen and prick tests in dogs with atopic dermatitis. Vet Dermatol. 2024 Feb;35(1):71-80. doi: 10.1111/vde.13209. Epub 2023 Sep 28. PMID: 37770410. 16: Ashton LV, Weishaar KM, Séguin B, MacNeill AL. Oclacitinib and Myxoma Virus Therapy in Dogs with High-Grade Soft Tissue Sarcoma. Biomedicines. 2023 Aug 23;11(9):2346. doi: 10.3390/biomedicines11092346. PMID: 37760788; PMCID: PMC10525839. 17: Mwacalimba K, Hillier A, Rosenbaum M, Brennan C, Amodie D. Diminished antimicrobial drug use in dogs with allergic dermatitis treated with oclacitinib. Front Vet Sci. 2023 Sep 7;10:1207582. doi: 10.3389/fvets.2023.1207582. PMID: 37745208; PMCID: PMC10512704. 18: Jasiecka-Mikołajczyk A, Maślanka T. Depletion of T and B cells in lymphoid tissues of mice induced by oclacitinib, a Janus kinase inhibitor. Pol J Vet Sci. 2023 Sep 20;26(3):431-440. doi: 10.24425/pjvs.2023.145049. PMID: 37727128. 19: Hernandez-Bures A, Bidot WA, Griffin CE, Rosenkrantz WS. The use of oclacitinib compared to azathioprine in the management of canine pemphigus foliaceus: A retrospective analysis. Vet Dermatol. 2023 Dec;34(6):554-566. doi: 10.1111/vde.13203. Epub 2023 Sep 12. PMID: 37700599. 20: Motz AK, St Germaine LL, Hoffmann DE, Sung J. A retrospective evaluation of the effect of oclacitinib (Apoquel) administration on development of surgical site infection following clean orthopedic stifle surgery. PLoS One. 2023 Aug 9;18(8):e0289827. doi: 10.1371/journal.pone.0289827. PMID: 37556416; PMCID: PMC10411735.