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Brepocitinib (PF-06700841) JAK inhibitor

Name: Brepocitinib (PF-06700841)
Brand: Selleck Chemicals
SKU: S8804
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S8804

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.

Chemical Structure

Molecular Weight: 389.40

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS/MSDS
Datasheet

98.10

Related Targets	EGFR STAT Pim
Other JAK Inhibitors	BMS-986165 (Deucravacitinib) AZD1480 WP1066 Filgotinib (GLPG0634) Momelotinib (CYT387) AT9283 Gandotinib (LY2784544) Pacritinib (SB1518) NVP-BSK805 2HCl TG101209

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (200.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 78 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.900mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 78 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.970mg/ml (2.49mM)	Taking the 1 mL working solution as an example, add 50 μL of 19.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	389.40	Formula	C₁₈H₂₁F₂N₇O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1883299-62-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	PF-841			SMILES	CN1C=C(C=N1)NC2=NC=CC(=N2)N3CC4CCC(C3)N4C(=O)C5CC5(F)F

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	JAK1 (Cell-free assay) 17 nM Tyk2 (Cell-free assay) 23 nM JAK2 (Cell-free assay) 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/30113844/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-27)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06978725	RECRUITING	Cutaneous Sarcoidosis	Priovant Therapeutics, Inc.	2025-04-09	PHASE2; PHASE3
NCT07532603	RECRUITING	Lichen Planopilaris	Priovant Therapeutics, Inc.	2026-03-19	PHASE2; PHASE3
NCT06431373	ACTIVE_NOT_RECRUITING	Uveitis, Posterior; Uveitis, Intermediate; Uveitis	Priovant Therapeutics, Inc.	2024-09-11	PHASE3
NCT05437263	ACTIVE_NOT_RECRUITING	Dermatomyositis	Priovant Therapeutics, Inc.	2022-10-31	PHASE3
NCT06433999	COMPLETED	Dermatomyositis; Dermatomyositis, Adult Type	Priovant Therapeutics, Inc.	2024-08-28	PHASE2
NCT05523765	COMPLETED	Non-infectious Intermediate Uveitis; Non-infectious Posterior Uveitis; Non-infectious Pan Uveitis	Priovant Therapeutics, Inc.	2022-11-14	PHASE2

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