A JAK family kinase inhibitor (IC50s = 10

Oclacitinib – 1 mg

Brand:
Cayman
CAS:
1208319-26-9
Storage:
-20
UN-No:
Non-Hazardous - /

Oclacitinib is an inhibitor of the JAK family kinases JAK1, JAK2, JAK3, and TYK2 (IC50s = 10, 18, 99, and 84 nM, respectively).{30396} 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.{48761} 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.  

 

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Description

A JAK family kinase inhibitor (IC50s = 10, 18, 99, and 84 nM for JAK1, JAK2, JAK3, and TYK2, respectively); selective for JAK kinases over a panel of 38 additional kinases at 1 μM; inhibits LPS-induced increases in IL-12 and TNF-α levels in murine BMDCs in a concentration-dependent manner; topical administration 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 TDI-induced allergic dermatitis at 0.1, 0.25, and 0.5%

Formal name: trans-N-methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-cyclohexanemethanesulfonamide

Synonyms:  PF-03394197

Molecular weight: 337.4

CAS: 1208319-26-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|JAK Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|JAK Signaling||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity

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