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Peficitinib JAK inhibitor

Name: Peficitinib
Brand: Selleck Chemicals
SKU: S7650
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S7650

Peficitinib is an orally bioavailable JAK inhibitor. Phase 3.

Chemical Structure

Molecular Weight: 326.39

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

Quality Control

Batch: Purity: 99.69%

99.69

Related Targets	EGFR STAT Pim
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Chemical Information, Storage & Stability

Molecular Weight	326.39	Formula	C₁₈H₂₂N₄O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	944118-01-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ASP015K, JNJ-54781532			Smiles	C1C2CC3CC(C2)(CC1C3NC4=C5C=CNC5=NC=C4C(=O)N)O

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.250mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL 65 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	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]
References	https://pubmed.ncbi.nlm.nih.gov/28117214/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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