PF-03394197

• CAT Number: I008397
• CAS Number: 1208319-26-9
• Molecular Formula: C₁₅H₂₃N₅O₂S
• Molecular Weight: 337.44
• Purity: ≥95%
• Target: JNK
• Solubility: Soluble in DMSO, not in water
• Storage: Store at -20°C
• IUPAC Name: N-methyl-1-[4-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexyl]methanesulfonamide
• InChI: 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)
• InChIKey: HJWLJNBZVZDLAQ-UHFFFAOYSA-N
• SMILES: CNS(=O)(=O)CC1CCC(CC1)N(C)C2=NC=NC3=C2C=CN3

Oclacitinib (Cat.No:I008397), 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.

Reference

1:The frequency of urinary tract infection and subclinical bacteriuria in dogs with allergic dermatitis treated with oclacitinib: a prospective study. Simpson AC, Schissler JR, Rosychuk RAW, Moore AR.Vet Dermatol. 2017 May 17. doi: 10.1111/vde.12450. [Epub ahead of print] PMID: 28513001 2:Demonstration of rebound phenomenon following abrupt withdrawal of the JAK1 inhibitor oclacitinib. Fukuyama T, Ganchingco JR, Bäumer W.Eur J Pharmacol. 2017 Jan 5;794:20-26. doi: 10.1016/j.ejphar.2016.11.020. Epub 2016 Nov 12. PMID: 27847179 3:Repeated oral dose tolerance in dogs treated concomitantly with ciclosporin and oclacitinib for three weeks. Panteri A, Strehlau G, Helbig R, Prost C, Doucette K.Vet Dermatol. 2016 Feb;27(1):22-e7. doi: 10.1111/vde.12278. Epub 2015 Dec 11. PMID: 26660461 Free PMC Article4:Aggression behaviour induced by oral administration of the Janus-kinase inhibitor tofacitinib, but not oclacitinib, under stressful conditions. Fukuyama T, Tschernig T, Qi Y, Volmer DA, Bäumer W.Eur J Pharmacol. 2015 Oct 5;764:278-82. doi: 10.1016/j.ejphar.2015.06.060. Epub 2015 Jul 9. PMID: 26164790 5:Topically Administered Janus-Kinase Inhibitors Tofacitinib and Oclacitinib Display Impressive Antipruritic and Anti-Inflammatory Responses in a Model of Allergic Dermatitis. Fukuyama T, Ehling S, Cook E, Bäumer W.J Pharmacol Exp Ther. 2015 Sep;354(3):394-405. doi: 10.1124/jpet.115.223784. Epub 2015 Jul 9. PMID: 26159873 Free Article6:Oclacitinib in feline nonflea-, nonfood-induced hypersensitivity dermatitis: results of a small prospective pilot study of client-owned cats. Ortalda C, Noli C, Colombo S, Borio S.Vet Dermatol. 2015 Aug;26(4):235-e52. doi: 10.1111/vde.12218. Epub 2015 May 4. PMID: 25940959 7:Long-term compassionate use of oclacitinib in dogs with atopic and allergic skin disease: safety, efficacy and quality of life. Cosgrove SB, Cleaver DM, King VL, Gilmer AR, Daniels AE, Wren JA, Stegemann MR.Vet Dermatol. 2015 Jun;26(3):171-9, e35. doi: 10.1111/vde.12194. Epub 2015 Feb 16. PMID: 25688708 8:A blinded, randomized clinical trial comparing the efficacy and safety of oclacitinib and ciclosporin for the control of atopic dermatitis in client-owned dogs. Little PR, King VL, Davis KR, Cosgrove SB, Stegemann MR.Vet Dermatol. 2015 Feb;26(1):23-30, e7-8. doi: 10.1111/vde.12186. Epub 2014 Dec 12. PMID: 25496303 Free PMC Article9:Efficacy of oclacitinib (Apoquel®) compared with prednisolone for the control of pruritus and clinical signs associated with allergic dermatitis in client-owned dogs in Australia. Gadeyne C, Little P, King VL, Edwards N, Davis K, Stegemann MR.Vet Dermatol. 2014 Dec;25(6):512-8, e86. doi: 10.1111/vde.12166. Epub 2014 Aug 11. PMID: 25109820 Free PMC Article10:A blinded, randomized, placebo-controlled trial of the efficacy and safety of the Janus kinase inhibitor oclacitinib (Apoquel®) in client-owned dogs with atopic dermatitis. Cosgrove SB, Wren JA, Cleaver DM, Walsh KF, Follis SI, King VI, Tena JK, Stegemann MR.Vet Dermatol. 2013 Dec;24(6):587-97, e141-2. doi: 10.1111/vde.12088. PMID: 24581322 Free PMC Article