Shopping Cart

Your shopping cart is currently empty

Brepocitinib

Name: Brepocitinib
Brand: TargetMol
SKU: TQ0010
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

😃Good

Catalog No. TQ0010Cas No. 1883299-62-4

Alias PF-06700841

Brepocitinib (PF-06700841) is a potent dual JAK1/TYK2 inhibitor with IC50 values of 17 nM and 23 nM, respectively, and also inhibits JAK2 and JAK3 with IC50 values of 77 nM and 6.49 μM.

Brepocitinib

Copy Product Info

😃Good

Purity: 99.82%

Catalog No. TQ0010Alias PF-06700841Cas No. 1883299-62-4

Brepocitinib (PF-06700841) is a potent dual JAK1/TYK2 inhibitor with IC50 values of 17 nM and 23 nM, respectively, and also inhibits JAK2 and JAK3 with IC50 values of 77 nM and 6.49 μM.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
2 mg	$40	In Stock	In Stock
5 mg	$64	In Stock	In Stock
10 mg	$106	In Stock	In Stock
25 mg	$228	In Stock	In Stock
50 mg	$413	In Stock	In Stock
100 mg	$662	In Stock	In Stock
200 mg	$926	-	In Stock
1 mL x 10 mM (in DMSO)	$71	In Stock	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

Select Batch

Purity:99.82%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	Brepocitinib (PF-06700841) is a potent dual JAK1/TYK2 inhibitor with IC50 values of 17 nM and 23 nM, respectively, and also inhibits JAK2 and JAK3 with IC50 values of 77 nM and 6.49 μM.
Targets&IC50	JAK1:17 nM (cell free), JAK2:77 nM (cell free), TYK2:23 nM (cell free), JAK3:6.9 μM
In vitro	PF-06700841 inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (human whole blood IC50s: 65/120 nM). PF-06700841 inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (IC50s: 238/204 nM). PF-06700841 also has good potency against IL6/pStat1 in the CD3+ cellular subset (IC50: 81 nM), but lower inhibition of IL6/pSTAT3, again in the CD3+ cellular subset (IC50: 641 nM). PF-06700841 inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34+ progenitor cells (IC50: 577 nM). IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by PF-06700841 (IC50s: 305 nM/86 nM).
In vivo	PF-06700841 (3-30 mg/kg; p.o; for 7 consecutive days; female Lewis rats) treatment significantly reduces paw volume increase in a dose-dependent manner. The plasma concentrations in animals dosed with PF-06700841 at peak (30 min) and trough (24 h) time intervals post final dose respectively are as follows: 3 mg/kg, 3.54 μM, 0.0221 μM; 10 mg/kg, 10.95 μM, 0.06 μM; and 30 mg/kg, 23.89 μM, 0.06 μM.
Synonyms	PF-06700841

Chemical Properties

Molecular Weight	389.4
Formula	C₁₈H₂₁F₂N₇O
Cas No.	1883299-62-4
Smiles	C(=O)(N1C2CN(CC1CC2)C3=NC(NC=4C=NN(C)C4)=NC=C3)[C@H]5C(F)(F)C5
Relative Density.	1.63 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 75 mg/mL (192.6 mM), Sonication is recommended.

DMSO: 150 mg/mL (385.21 mM), Sonication is recommended.

H2O: Insoluble

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5681 mL	12.8403 mL	25.6805 mL	128.4027 mL
5 mM	0.5136 mL	2.5681 mL	5.1361 mL	25.6805 mL
10 mM	0.2568 mL	1.2840 mL	2.5681 mL	12.8403 mL
20 mM	0.1284 mL	0.6420 mL	1.2840 mL	6.4201 mL
50 mM	0.0514 mL	0.2568 mL	0.5136 mL	2.5681 mL
100 mM	0.0257 mL	0.1284 mL	0.2568 mL	1.2840 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc