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

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.


Price and Availability

Size
Price

10mg
USD 90
100mg
USD 450
1g
USD 2450
Size
Price

25mg
USD 150
200mg
USD 850
2g
USD 3850
Size
Price

50mg
USD 250
500mg
USD 1450
5g
USD 5950

Oclacitinib, purity > 98%, is in stock. The same day shipping out after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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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


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


Technical Data

Appearance:
white to off-white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (MSDS):

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).

Harmonized System Code:
293490


References

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.