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 No. 1622902-68-4

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

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
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

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


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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