Peficitinib (ASP015K)

Catalog No.S7650 Synonyms: JNJ-54781532

For research use only.

Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.

Peficitinib (ASP015K) Chemical Structure

CAS No. 944118-01-8

Purity & Quality Control

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Biological Activity

Description Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
Targets
JAK [1]
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]

In vivo In the rat AIA model, ASP015K (p.o.) significantly decreases paw swelling and ankle bone destruction score. [1]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 326.39
Formula

C18H22N4O2

CAS No. 944118-01-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1C2CC3CC(C2)(CC1C3NC4=C5C=CNC5=NC=C4C(=O)N)O

In vivo Formulation Calculator (Clear solution)

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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.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02760342 Completed Drug: peficitinib|Drug: Metformin Healthy Subjects Astellas Pharma Inc May 15 2016 Phase 1
NCT02586194 Completed Drug: ASP015K Patients With Impaired Hepatic Function Astellas Pharma Inc December 28 2015 Phase 1
NCT02603497 Completed Drug: ASP015K Patients With Impaired Renal Function Astellas Pharma Inc November 24 2015 Phase 1
NCT02531191 Completed Drug: peficitinib Healthy Volunteers Astellas Pharma Inc June 21 2015 Phase 1
NCT02117505 Completed Drug: Formulation 2|Drug: Formulation 1 Healthy Janssen Research & Development LLC April 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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