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Brepocitinib

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

🥰Excellent

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

🥰Excellent

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	Availability
1 mg	$30	In Stock
5 mg	$68	In Stock
10 mg	$112	In Stock
25 mg	$238	In Stock
50 mg	$433	In Stock
100 mg	$695	In Stock
200 mg	$965	In Stock
1 mL x 10 mM (in DMSO)	$74	In Stock

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Purity:99.82%

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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	TYK2:23 nM (cell free), JAK3:6.9 μM, JAK1:17 nM (cell free), JAK2:77 nM (cell free)
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: 75 mg/mL (192.6 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

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In Vivo Formulation Calculator (Clear solution)

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

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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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