Brepocitinib (PF-06700841)

Catalog No.S8804 Synonyms: PF-841

For research use only.

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

CAS No. 1883299-62-4

Purity & Quality Control

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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

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].

Protocol (from reference)

Animal Research:

[1]

  • 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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 389.40
Formula

C18H21F2N7O

CAS No. 1883299-62-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C=C(C=N1)NC2=NC=CC(=N2)N3CC4CCC(C3)N4C(=O)C5CC5(F)F

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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.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05076006 Recruiting Drug: PF-06700841|Drug: Placebo Cicatricial Alopecia Emma Guttman|Pfizer|Icahn School of Medicine at Mount Sinai May 21 2021 Phase 2
NCT04260464 Completed Drug: PF-06700841 Healthy Volunteer|Renal Impairment Pfizer July 3 2020 Phase 1
NCT04090047 Completed Drug: PF-06700841|Drug: Itraconazole Heathy Participants Pfizer September 24 2019 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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