WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 510286
Description: 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.
MedKoo Cat#: 510286
Chemical Formula: C15H23N5O2S
Exact Mass: 337.15725
Molecular Weight: 337.44
Elemental Analysis: C, 53.39; H, 6.87; N, 20.75; O, 9.48; S, 9.50
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
1: Little PR, King VL, Davis KR, Cosgrove SB, Stegemann MR. A blinded, randomized clinical trial comparing the efficacy and safety of oclacitinib and ciclosporin for the control of atopic dermatitis in client-owned dogs. Vet Dermatol. 2014 Dec 12. doi: 10.1111/vde.12186. [Epub ahead of print] PubMed PMID: 25496303.
2: Gadeyne C, Little P, King VL, Edwards N, Davis K, Stegemann MR. 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. Vet Dermatol. 2014 Dec;25(6):512-e86. doi: 10.1111/vde.12166. Epub 2014 Aug 11. PubMed PMID: 25109820.
3: Cosgrove SB, Wren JA, Cleaver DM, Walsh KF, Follis SI, King VI, Tena JK, Stegemann MR. 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. Vet Dermatol. 2013 Dec;24(6):587-97, e141-2. doi: 10.1111/vde.12088. PubMed PMID: 24581322.
4: 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. PubMed PMID: 24495176.
5: Collard WT, Hummel BD, Fielder AF, King VL, Boucher JF, Mullins MA, Malpas PB, Stegemann MR. The pharmacokinetics of oclacitinib maleate, a Janus kinase inhibitor, in the dog. J Vet Pharmacol Ther. 2014 Jun;37(3):279-85. doi: 10.1111/jvp.12087. Epub 2013 Dec 16. PubMed PMID: 24330031.
6: 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. PubMed PMID: 23829933.