A JAK family kinase inhibitor
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Labeled Version(s)
28808Oclacitinib-13C-d3
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Oclacitinib

Item No. 18722

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
trans-N-methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-cyclohexanemethanesulfonamide
CAS Number
1208319-26-9
Synonyms
  • PF-03394197
Molecular Formula
C15H23N5O2S
Formula Weight
337.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 14 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 12 mg/ml
λmax
217, 286 nm
SMILES
CNS(C[C@@H]1CC[C@@H](N(C2=NC=NC3=C2C=CN3)C)CC1)(=O)=O
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-
InChi Key
HJWLJNBZVZDLAQ-HAQNSBGRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    50 mg

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    Product Description

    Oclacitinib is an inhibitor of the JAK family kinases JAK1, JAK2, JAK3, and TYK2 (IC50s = 10, 18, 99, and 84 nM, respectively).1 It is selective for JAK kinases over a panel of 38 additional kinases at 1 μM. Oclacitinib inhibits LPS-induced increases in IL-12 and TNF-α levels in murine bone marrow-derived dendritic cells (BMDCs) in a concentration-dependent manner.2 Topical administration of oclacitinib (0.1, 0.25, and 0.5%) reduces scratching behavior and ear edema, as well as decreases levels of IL-1β, IL-4, and IL-6 in ear skin, in a mouse model of allergic dermatitis induced by toluene-2,3-diisocyanate (TDI). Formulations containing oclacitinib have been used in the treatment of pruritus associated with allergic dermatitis and the control of atopic dermatitis in dogs.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gonzales, A.J., Bowman, J.W., Fici, G.J., et al. Oclacitinib (APOQUEL®) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. J. Vet. Pharmacol. Ther. 37(4), 317-324 (2014).

    2. Fukuyama, T., Ehling, S., Cook, E., et al. Topically administered Janus-kinase inhibitors ofacitinib and olacitinib dsplay impressive antipruritic and anti-inflammatory responses in a model of allergic dermatitis. J. Pharmacol. Exp. Ther. 354(3), 394-405 (2015).