Cat. No.: HY-112708A

Brepocitinib P-Tosylate

(Synonyms: PF-06700841 P-Tosylate)

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

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.

Purity: 99.99%
CAS No.: 2140301-96-6
Formula: C₂₅H₂₉F₂N₇O₄S
Molecular Weight:561.60

Storage:

4°C, sealed storage, away from moisture

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

Brepocitinib P-Tosylate Chemical Structure

CAS No.: 2140301-96-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

JAK1

17 nM (IC₅₀)

JAK2

77 nM (IC₅₀)

JAK3

6.9 μM (IC₅₀)

All JAK Isoforms :

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2140301-96-6
Appearance Solid
Molecular Weight 561.60
Formula C₂₅H₂₉F₂N₇O₄S
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
Synonyms

PF-06700841 P-Tosylate
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)

Publications (3)

All RT-PCRWBCell Proliferation/Viability AssayCell Migration/Invasion Assay

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Journal Impact Factor

J Exp Clin Cancer Res

Unveiling the role of HP1α-HDAC1-STAT1 axis as a therapeutic target for HP1α-positive intrahepatic cholangiocarcinoma. [Abstract]

2024 May 30;43(1):152. PMID: 38812060

Brepocitinib P-Tosylate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 May 30;43(1):152. [Abstract]

Brepocitinib (PF-06700841; 50 nM; 24 h) inhibited mRNA expression of p-STAT1, STAT1, and ISG expression by HP1α knockdown in HUCCT1 and HCCC-9810 cells.

Brepocitinib P-Tosylate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 May 30;43(1):152. [Abstract]

Brepocitinib (PF-06700841; 50 nM; 24 h) inhibited protein expression of p-STAT1, STAT1, and ISG by HP1α knockdown in HUCCT1 and HCCC-9810 cells.
Inflamm Bowel Dis

Clinical and Mechanistic Characteristics of Current JAK Inhibitors in IBD. [Abstract]

2021 Oct 18;27(10):1674-1683. PMID: 33295611
Heliyon

Hyperin promotes proliferation, migration, and invasion of HTR-8/SVneo trophoblast cells via activation of JAK1/STAT3 pathway in recurrent spontaneous abortions. [Abstract]

2023 Jan 13;9(1):e12958. PMID: 36747955

Brepocitinib P-Tosylate purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958. [Abstract]

PF-06700841 (Brepocitinib; 20 nM; 24 h) blocks hyperin-induced expression of JAK1 and STAT3 in HTR-8/SVneo cells.

Brepocitinib P-Tosylate purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958. [Abstract]

Brepocitinib (PF-06700841; 20 nM; 24 h) blocked hyperin induced JAK1 and STAT3 mRNA expression in HTR8/SVneo cells.

Brepocitinib P-Tosylate purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958. [Abstract]

Brepocitinib (PF-06700841; 20 nM; 12, 24, 36, 48 h) blocked the effects of hyperin on cell proliferation in HTR8/SVneo cells.

Brepocitinib P-Tosylate purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958. [Abstract]

Brepocitinib (PF-06700841; 20 nM; 12, 24, 36, 48 h) blocked the protein expression of Ki67, MCM2, MMP2, MMP9, VEGFA, and PCNA in HTR8/SVneo cells.

Brepocitinib P-Tosylate purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958. [Abstract]

Brepocitinib (PF-06700841; 20 nM; 48 h) inhibited the effect of hyperin on HTR-8/SVneo cell migration.

Brepocitinib P-Tosylate purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958. [Abstract]

Brepocitinib (PF-06700841; 20 nM; 48 h) inhibited the invasion ability in HTR-8/SVneo cells.

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)

H₂O : 2 mg/mL (3.56 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	1.7806 mL	8.9031 mL	17.8063 mL	44.5157 mL
DMSO	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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Brepocitinib P-Tosylate

3 Cited Publications

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Brepocitinib P-Tosylate

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Publications Citing Use of MedChemExpress (MCE) Brepocitinib P-Tosylate

All JAK Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Brepocitinib P-Tosylate Related Classifications

HY-112708A Related Classifications