Oclacitinib maleate

Catalog No.S8195 Synonyms: PF-03394197

Oclacitinib maleate Chemical Structure

Molecular Weight(MW): 453.51

Oclacitinib is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which did not inhibit a panel of 38 non-JAK kinases.

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Biological Activity

Description Oclacitinib is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which did not inhibit a panel of 38 non-JAK kinases.
Targets
JAK1 [1]
(Cell-free assay)
JAK2 [1]
(Cell-free assay)
TYK2 [1]
(Cell-free assay)
JAK3 [1]
(Cell-free assay)
10nM 18nM 84nM 99nM
In vitro

PF-03394197 inhibits JAK family members by 50% at concentrations ranging from 10 to 99 nM and does not inhibit a panel of 38 non-JAK kinases. PF-03394197 is most potent at inhibiting JAK1. PF-03394197 also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation as well as pruritus. PF-03394197 has minimal effects on cytokines which does not activate the JAK1 enzyme in cells[1].

In vivo PF-03394197 administered orally at a dose of 0.4–0.6 mg/kg twice daily is safe and efficacious in controlling the pruritus associated with allergic dermatitis. PF-03394197 provides itch relief within 24 h that persistes through the treatment period, with over 70% of the treated dogs achieving a >50% reduction in pruritus by day 7[2].

Protocol

Solubility (25°C)

In vitro DMSO 90 mg/mL (198.45 mM)
Ethanol 90 mg/mL (198.45 mM)
Water 18 mg/mL (39.69 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 453.51
Formula

C15H23N5O2S.C4H4O4

CAS No. 1640292-55-2
Storage powder
Synonyms PF-03394197

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID