Home JAK/STAT JAK inhibitor Oclacitinib maleate

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Oclacitinib maleate JAK inhibitor

Cat.No.S8195

Oclacitinib maleate (PF-03394197) 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. It does not inhibit a panel of 38 non-JAK kinases.
Oclacitinib maleate JAK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 453.51

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S819501 DMSO]90 mg/mL]false]Ethanol]90 mg/mL]false]Water]18 mg/mL]false Purity: 99.84%
99.84

Chemical Information, Storage & Stability

Molecular Weight 453.51 Formula

C15H23N5O2S.C4H4O4

 Storage (From the date of receipt)
CAS No. 1640292-55-2 Download SDF Storage of Stock Solutions

Synonyms PF-03394197 Smiles CNS(=O)(=O)CC1CCC(CC1)N(C)C2=NC=NC3=C2C=CN3.C(=CC(=O)O)C(=O)O

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (198.45 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 90 mg/mL

Water : 18 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
JAK1 [1]
(Cell-free assay)
10nM
JAK2 [1]
(Cell-free assay)
18nM
TYK2 [1]
(Cell-free assay)
84nM
JAK3 [1]
(Cell-free assay)
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].
References

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