Home JAK/STAT JAK inhibitor Abrocitinib (PF-04965842) For research use only.

Abrocitinib (PF-04965842)

Abrocitinib (PF-04965842) is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively.

Abrocitinib (PF-04965842) Chemical Structure

Abrocitinib (PF-04965842) Chemical Structure

CAS: 1622902-68-4

Selleck's Abrocitinib (PF-04965842) has been cited by 4 publications

Purity & Quality Control

Batch: S876501 DMSO] 65 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.45%
99.45

Abrocitinib (PF-04965842) Related Products

Signaling Pathway

JAK Signaling Pathways

JAK Signaling Pathway

Choose Selective JAK Inhibitors

Biological Activity

Description Abrocitinib (PF-04965842) is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively.
Targets
JAK1 [1]
(Cell-free assay)		 JAK2 [1]
(Cell-free assay)		 TYK2 [1]
(Cell-free assay)
29 nM 803 nM 1.253 μM
In vitro
In vitro

Abrocitinib (PF-04965842) is a potent JAK inhibitor with IC50 of 29 and 803 nM for JAK1 and JAK2, respectively.
In Vivo
In vivo

Physicochemical properties and pharmacokinetic parameters of PF-04965842 are examined in rats following doses of 1 mg/kg iv or 3 mg/kg po. Clearance of PF-04965842 is low relative to total liver blood flow (CL = 26.6 mL/min/kg). Vdss = 1.04 L/kg. T1/2 = 1.1 h. The oral availability of PF-04965842 is 95.6%. PF-04965842 demonstrates efficacy in a dose-responsive manner in a therapeutic rat adjuvant-induced arthritis model[1].
Animal Research Animal Models Female Lewis rats (8−10 weeks old)
Dosages 50, 15, 5 and 0.5 mg/kg
Administration via oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04065633 Completed
Dermatitis Atopic
Pfizer
 July 18 2019 Phase 1
NCT03937258 Completed
Healthy
Pfizer
 May 21 2019 Phase 1
NCT03796676 Completed
Atopic Dermatitis
Pfizer
 February 18 2019 Phase 3
NCT03660241 Completed
Renal Impairment
Pfizer
 October 5 2018 Phase 1
NCT03626415 Completed
Hepatic Impairment
Pfizer
 October 1 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 323.41 Formula

C14H21N5O2S
CAS No. 1622902-68-4 SDF --
Smiles CCCS(=O)(=O)NC1CC(C1)N(C)C2=NC=NC3=C2C=CN3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 65 mg/mL ( (200.98 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)

mg/kg g μL

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.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Abrocitinib (PF-04965842) | Abrocitinib (PF-04965842) supplier | purchase Abrocitinib (PF-04965842) | Abrocitinib (PF-04965842) cost | Abrocitinib (PF-04965842) manufacturer | order Abrocitinib (PF-04965842) | Abrocitinib (PF-04965842) distributor