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

Name: Brepocitinib P-Tosylate
Brand: MedChemExpress
SKU: HY-112708A
Rating: 5.0 (3 reviews)

Cat. No.: HY-112708A Purity: 99.99%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 2140301-96-6

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
1 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
250 mg	해외재고보유	Estimated Time of Arrival: December 31
500 mg	견적 받기
1 g	견적 받기

or 대량구매 문의

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 3 publication(s) in Google Scholar

Other Forms of Brepocitinib P-Tosylate:

Brepocitinib In-stock

3 Publications Citing Use of MCE Brepocitinib P-Tosylate

: Brepocitinib P-Tosylate purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958.; PF-06700841 (Brepocitinib; 20 nM; 24 h) blocks hyperin-induced expression of JAK1 and STAT3 in HTR-8/SVneo cells.

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View All JAK Isoform Specific Products:

View All Isoforms

JAK1 JAK2 JAK3 Tyk2 JAK

Biological Activity
순도&문서
References
고객리뷰

제품 설명

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

분자량

561.60

화학식

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

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, sealed storage, away from moisture

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

용액&용해도

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)

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.

* 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.

몰농도 계산기
농도 희석 계산기

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.

순도&문서

Purity: 99.99%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (253 KB) HNMR (273 KB) LCMS (120 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

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.

Brepocitinib P-Tosylate Related Classifications

Inflammation/Immunology

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)

고객리뷰

Other Forms of Brepocitinib P-Tosylate:

Brepocitinib P-Tosylate Related Antibodies

3 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

순도&문서

References

고객리뷰

Brepocitinib P-Tosylate Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Brepocitinib P-Tosylate Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report