Oclacitinib
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MedKoo CAT#: 510286

CAS#: 1208319-26-9

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.


Chemical Structure

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Oclacitinib
CAS# 1208319-26-9

Theoretical Analysis

MedKoo Cat#: 510286
Name: Oclacitinib
CAS#: 1208319-26-9
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

Price and Availability

Size Price Availability Quantity
10.0mg USD 90.0 Ready to ship
25.0mg USD 150.0 Ready to ship
50.0mg USD 250.0 Ready to ship
100.0mg USD 450.0 Ready to ship
200.0mg USD 850.0 Ready to ship
500.0mg USD 1450.0 Ready to ship
1.0g USD 2450.0 Ready to ship
2.0g USD 3850.0 Ready to ship
5.0g USD 5950.0 2 Weeks
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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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 12.0 35.6

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.

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

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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.