PF-06700841 P-Tosylate (Synonyms: PF-06700841 P-Tosylate) |
Catalog No.GC19405
One-Click Copy Product Info
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PF-06700841 P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50 values of 17nM and 23nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2140301-96-6
Sample solution is provided at 25 µL, 10mM.
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PF-06700841 P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50 values of 17nM and 23nM, respectively [1]. PF-06700841 P-Tosylate inhibits JAK-dependent signaling at multiple points in the pathogenic cycle, including keratinocyte signaling, maintenance of inflammatory T-cell infiltrate, and direct inhibition of TYK2-dependent IL-23 signaling[2]. PF-06700841 P-Tosylate has been widely used to attenuate both cutaneous and muscular inflammation in different models[3].
In vitro, PF-06700841 P-Tosylate pretreatment at 10µM for 1h inhibited IFNγ-induced nitrite production and cytokine transcription in Raw264.7 cells[4]. PF-06700841 P-Tosylate (20nM) treatment for 24h significantly inhibited the proliferation, migration, and invasion effects of hyperin on HTR-8/SVneo cells[5].
In vivo, PF-06700841 P-Tosylate treatment via oral administration at a dose of 3mg/kg/day for 3 days significantly mitigated lipopolysaccharide (LPS)-induced neutrophil inflammation in mice[6]. Oral administration of PF-06700841 P-Tosylate at a dose of 30mg/kg/day for 3 consecutive days significantly alleviated disease severity in a rat model of adjuvant-induced arthritis (AIA)[7].
References:
[1] Li Y, Chen J, Bolinger A A, et al. Target-based small molecule drug discovery towards novel therapeutics for inflammatory bowel diseases[J]. Inflammatory bowel diseases, 2021, 27(Supplement_2): S38-S62.
[2] Page K M, Suarez-Farinas M, Suprun M, et al. Molecular and cellular responses to the TYK2/JAK1 inhibitor PF-06700841 reveal reduction of skin inflammation in plaque psoriasis[J]. Journal of Investigative Dermatology, 2020, 140(8): 1546-1555. e4.
[3] Krueger J G, McInnes I B, Blauvelt A. Tyrosine kinase 2 and Janus kinase‒signal transducer and activator of transcription signaling and inhibition in plaque psoriasis[J]. Journal of the American Academy of Dermatology, 2022, 86(1): 148-157.
[4] Romero-Ramírez L, García-Rama C, Mey J. Janus kinase inhibitor brepocitinib rescues myelin phagocytosis under inflammatory conditions: in vitro evidence from microglia and macrophage cell lines[J]. Molecular Neurobiology, 2024, 61(9): 6423-6434.
[5] Mu Z, Shen S, Tang L, et al. Hyperin promotes proliferation, migration, and invasion of HTR-8/SVneo trophoblast cells via activation of JAK1/STAT3 pathway in recurrent spontaneous abortions[J]. Heliyon, 2023, 9(1).
[6] Nayak B B, Bärnthaler T, Rajesh R, et al. Brepocitinib, a selective TYK2/JAK1 inhibitor, mitigates neutrophilic inflammation and glucocorticoid receptor-β expression in COPD[J]. American Journal of Physiology-Lung Cellular and Molecular Physiology, 2026.
[7] Fensome A, Ambler C M, Arnold E, 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-06700841)[J]. Journal of medicinal chemistry, 2018, 61(19): 8597-8612.
| Cell experiment [1]: | |
Cell lines | Raw264.7 cells |
Preparation Method | HepG2 cells were cultured in DMEM medium supplemented with 5% heat-inactivated fetal bovine serum, 100units /ml penicillin, and 100µg/ml streptomycin at 37°C in a 5% CO2 incubator. HepG2 cells were seeded at a density of 6×104 cells/well in 96-well flat-bottom plates and cultured in DMEM medium containing 1% FBS for 24 hours. Cells were pretreated with PF-06700841 P-Tosylate (0.01, 0.05, 0.2, 1, and 10µM) at 1h before adding IFNγ (10ng/ml) and exposure for 24h. Nitrite production and cytokine expression were analyzed. |
Reaction Conditions | 0.01, 0.05, 0.2, 1, and 10µM; 1h |
Applications | PF-06700841 P-Tosylate treatment inhibited IFNγ-induced nitrite production and cytokine transcription in Raw264.7 cells. |
| Animal experiment [2]: | |
Animal models | Female C57BL/6 mice |
Preparation Method | 8-week-old female C57BL/6 mice were housed in a specific pathogen-free (SPF) animal house maintained at 23°C with a 12h light/dark cycle and free access to water and food. Mice received intranasal LPS (5µg) or saline (vehicle control) to induce acute lung inflammation, along with oral PF-06700841 P-Tosylate (3mg/kg) or saline, once daily for three days. On day 4, the mice were sacrificed under anesthesia induced with ketamine (10mg/ml) and xylazine (1mg/ml). Then, bronchoalveolar lavage fluid (BALF) and blood samples were collected for analysis. |
Dosage form | 3mg/kg/day for 3 days; p.o. |
Applications | PF-06700841 P-Tosylate treatment significantly mitigated LPS-induced neutrophil inflammation in mice. |
References: | |
| Cas No. | 2140301-96-6 | SDF | |
| Synonyms | PF-06700841 P-Tosylate | ||
| Chemical Name | ((S)-2,2-difluorocyclopropyl)(3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone 4-methylbenzenesulfonate | ||
| Canonical SMILES | O=C([C@H]1C(F)(F)C1)N2C3CN(C4=NC(NC5=CN(C)N=C5)=NC=C4)CC2CC3.OS(=O)(C6=CC=C(C)C=C6)=O | ||
| Formula | C25H29F2N7O4S | M.Wt | 561.61 |
| Solubility | DMSO : 62.5 mg/mL (111.29 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7806 mL | 8.903 mL | 17.806 mL |
| 5 mM | 356.1 μL | 1.7806 mL | 3.5612 mL |
| 10 mM | 178.1 μL | 890.3 μL | 1.7806 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)