Brepocitinib P-Tosylate (Synonyms: PF-06700841 P-Tosylate)

Name: Brepocitinib P-Tosylate
Brand: MedChemExpress
SKU: HY-112708A
Rating: 4.5 (3 reviews)

Cat. No.: HY-112708A Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

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Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC₅₀s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits JAK2 and JAK3 with IC₅₀s of 77 nM and 6.49 μM, respectively.

For research use only. We do not sell to patients.

Brepocitinib P-Tosylate Chemical Structure

CAS No. : 2140301-96-6

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 99	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 99	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 38	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 130	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
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Based on 3 publication(s) in Google Scholar

Other Forms of Brepocitinib P-Tosylate:

Brepocitinib In-stock

2 Publications Citing Use of MCE Brepocitinib P-Tosylate

: Brepocitinib P-Tosylate purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13.; PF-06700841 (Brepocitinib; 20 nM; 24 h) blocks hyperin-induced expression of JAK1 and STAT3 in HTR-8/SVneo cells.

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Biological Activity
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References
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Description

IC₅₀ & Target^[1]

JAK1

17 nM (IC₅₀)

JAK2

77 nM (IC₅₀)

JAK3

6.9 μM (IC₅₀)

In Vitro

Brepocitinib (Compound 23) potently inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (human whole blood (HWB) IC₅₀s of 65 and 120 nM, respectively). Brepocitinib has good potency against IL6/pStat1 in the CD3⁺ cellular subset (IC₅₀ of 81 nM), but lower inhibition of IL6/pSTAT3, again in the CD3⁺ cellular subset (IC₅₀ of 641 nM). Brepocitinib also inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (HWB IC₅₀s of 238 and 204 nM, respectively). Brepocitinib inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34⁺ progenitor cells (IC₅₀ of 577 nM). IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by Brepocitinib with IC₅₀s of 305 nM and 86 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Brepocitinib (Compound 23; 3-30 mg/kg; oral administration; 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 Brepocitinib 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Lewis rats with induced arthritis^[1]
Dosage:	3 mg/kg, 10 mg/kg, or 30 mg/kg
Administration:	Oral administration; for 7 consecutive days
Result:	Increased in paw volume was significantly lower and dose-dependent.

Clinical Trial

Molecular Weight

561.60

Formula

C₂₅H₂₉F₂N₇O₄S

CAS No.

2140301-96-6

Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1C(F)(F)C1)N2C3CN(C4=NC(NC5=CN(C)N=C5)=NC=C4)CC2CC3.O=S(C6=CC=C(C)C=C6)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (89.03 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7806 mL	8.9031 mL	17.8063 mL
5 mM	0.3561 mL	1.7806 mL	3.5613 mL
10 mM	0.1781 mL	0.8903 mL	1.7806 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.86%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (254 KB) HNMR (272 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[1]. Fensome A, et al. Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700 [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7806 mL	8.9031 mL	17.8063 mL	44.5157 mL
	5 mM	0.3561 mL	1.7806 mL	3.5613 mL	8.9031 mL
	10 mM	0.1781 mL	0.8903 mL	1.7806 mL	4.4516 mL
	15 mM	0.1187 mL	0.5935 mL	1.1871 mL	2.9677 mL
	20 mM	0.0890 mL	0.4452 mL	0.8903 mL	2.2258 mL
	25 mM	0.0712 mL	0.3561 mL	0.7123 mL	1.7806 mL
	30 mM	0.0594 mL	0.2968 mL	0.5935 mL	1.4839 mL
	40 mM	0.0445 mL	0.2226 mL	0.4452 mL	1.1129 mL
	50 mM	0.0356 mL	0.1781 mL	0.3561 mL	0.8903 mL
	60 mM	0.0297 mL	0.1484 mL	0.2968 mL	0.7419 mL
	80 mM	0.0223 mL	0.1113 mL	0.2226 mL	0.5564 mL

Brepocitinib P-Tosylate Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Brepocitinib P-Tosylate2140301-96-6PF-06700841 P-TosylateJAKJanus kinaseInhibitorinhibitorinhibit

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Brepocitinib P-Tosylate (Synonyms: PF-06700841 P-Tosylate)

Customer Review

Other Forms of Brepocitinib P-Tosylate:

Brepocitinib P-Tosylate Related Antibodies

2 Publications Citing Use of MCE Brepocitinib P-Tosylate

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All JAK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Brepocitinib P-Tosylate Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Brepocitinib P-Tosylate Related Classifications

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