Home JAK/STAT JAK inhibitor Abrocitinib (PF-04965842)

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Abrocitinib (PF-04965842) JAK inhibitor

Cat.No.S8765

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) JAK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 323.41

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (200.98 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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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.

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Chemical Information, Storage & Stability

Molecular Weight 323.41 Formula

C14H21N5O2S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1622902-68-4 -- Storage of Stock Solutions

Synonyms N/A Smiles CCCS(=O)(=O)NC1CC(C1)N(C)C2=NC=NC3=C2C=CN3

Mechanism of Action

Targets/IC50/Ki
JAK1
(Cell-free assay)
29 nM
JAK2
(Cell-free assay)
803 nM
TYK2
(Cell-free assay)
1.253 μM
In vitro

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

Abrocitinib (PF-04965842) was examined for its physicochemical properties and pharmacokinetic parameters in rats following doses of 1 mg/kg iv or 3 mg/kg po. Its clearance 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 this compound is 95.6%. It demonstrates efficacy in a dose-responsive manner in a therapeutic rat adjuvant-induced arthritis model.
References

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06353087 Not yet recruiting
Dermatitis Atopic|Dermatitis|Eczema|Skin Diseases|Immune System Diseases|Janus Kinase Inhibitors
Pfizer
 April 1 2024 --
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

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