Home JAK/STAT JAK inhibitor Peficitinib For research use only.

Peficitinib

Synonyms: ASP015K, JNJ-54781532

Peficitinib is an orally bioavailable JAK inhibitor. Phase 3.

Peficitinib Chemical Structure

Peficitinib Chemical Structure

CAS No. 944118-01-8

Purity & Quality Control

Peficitinib Related Products

Signaling Pathway

JAK Signaling Pathways

JAK Signaling Pathway

Biological Activity

Description Peficitinib is an orally bioavailable JAK inhibitor. Phase 3.
Targets
JAK [1]
In vitro
In vitro

ASP015K suppresses the IL-2-induced proliferation of human T cells with greater potency than EPO-induced proliferation of human erythroleukemia cells. In human whole blood, ASP015K inhibits STAT5 phosphorylation (pSTAT5). [1]
Cell Research Cell lines Rat splenocytes
Concentrations 10 nM
Incubation Time 3 days
Method

Splenocytes were then incubated with IL-2 and peficitinib at designated concentrations in 96-well tissue culture plates
In Vivo
In vivo

In the rat AIA model, ASP015K (p.o.) significantly decreases paw swelling and ankle bone destruction score. [1]
Animal Research Animal Models Female Lewis rats
Dosages 1, 3, 10, and 30 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02760342 Completed
Healthy Subjects
Astellas Pharma Inc
 May 15 2016 Phase 1
NCT02586194 Completed
Patients With Impaired Hepatic Function
Astellas Pharma Inc
 December 28 2015 Phase 1
NCT02603497 Completed
Patients With Impaired Renal Function
Astellas Pharma Inc
 November 24 2015 Phase 1
NCT02531191 Completed
Healthy Volunteers
Astellas Pharma Inc
 June 21 2015 Phase 1
NCT02117505 Completed
Healthy
Janssen Research & Development LLC
 April 2014 Phase 1

Chemical Information & Solubility

Molecular Weight 326.39 Formula

C18H22N4O2
CAS No. 944118-01-8 SDF Download Peficitinib SDF
Smiles C1C2CC3CC(C2)(CC1C3NC4=C5C=CNC5=NC=C4C(=O)N)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 65 mg/mL ( (199.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

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.

Handling Instructions

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