Home JAK/STAT JAK inhibitor Brepocitinib (PF-06700841) For research use only.

Brepocitinib (PF-06700841)

Synonyms: PF-841

Brepocitinib (PF-06700841, PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.

Brepocitinib (PF-06700841) Chemical Structure

Brepocitinib (PF-06700841) Chemical Structure

CAS No. 1883299-62-4

Purity & Quality Control

Batch: S880401 DMSO]78 mg/mL]false]Ethanol]78 mg/mL]false]Water]Insoluble]false Purity: 98.10%
98.10

Brepocitinib (PF-06700841) Related Products

Signaling Pathway

JAK Signaling Pathways

JAK Signaling Pathway

Biological Activity

Description Brepocitinib (PF-06700841, PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.
Targets
JAK1 [1]
(Cell-free assay)		 Tyk2 [1]
(Cell-free assay)		 JAK2 [1]
(Cell-free assay)
17 nM 23 nM 77 nM
In Vivo
In vivo

The pharmacokinetics of PF-06700841 are studied in Sprague−Dawley rats following intravenous and oral administration (1 and 3 mg/kg respectively) of the tosylate salt, where the compound shows a plasma clearance of 31 mL/min/kg, a volume of distribution of 2.0 L/kg, and oral bioavailability of 83%. Following the 3 mg/kg oral dose, the Cmax is 774 ng/mL and the AUC∞ is 1340 ng·h/mL. The high oral bioavailability indicates high absorption from the gut, consistent with its in vitro passive permeability properties and high solubility[1].
Animal Research Animal Models Rat adjuvant induced arthritis model (8−10 weeks old female Lewis rats)
Dosages 3, 10, or 30 mg/kg/day
Administration oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05076006 Completed
Cicatricial Alopecia
Emma Guttman|Pfizer|Icahn School of Medicine at Mount Sinai
 May 19 2021 Phase 2
NCT04260464 Completed
Healthy Volunteer|Renal Impairment
Pfizer
 July 3 2020 Phase 1
NCT04090047 Completed
Heathy Participants
Pfizer
 September 24 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 389.40 Formula

C18H21F2N7O
CAS No. 1883299-62-4 SDF --
Smiles CN1C=C(C=N1)NC2=NC=CC(=N2)N3CC4CCC(C3)N4C(=O)C5CC5(F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 78 mg/mL ( (200.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 78 mg/mL

Water : 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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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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