Art. -Nr.: HY-100754C

Ritlecitinib tosylate

(Synonyms: PF-06651600 tosylate)

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

Ritlecitinib (PF-06651600) tosylate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib tosylate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib tosylate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).

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Reinheit: 99.65%
CAS. Nr.: 2192215-81-7
Formel: C₂₂H₂₇N₅O₄S
Molecular Weight:457.55

Speicherung:

-20°C, sealed storage, away from moisture

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

Ritlecitinib tosylate Chemical Structure

CAS. Nr.: 2192215-81-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

JAK3

33.1 nM (IC₅₀)

IL-2

IL-4

IL7R

IL-15

STAT3

STAT5

STAT6

Alle JAK Isoform-spezifische Produkte anzeigen :

Alle Interleukin Related Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

In Vitro

Ritlecitinib tosylate inhibits IL-15 in peripheral blood mononuclear cells (PBMCs) and heparin treated human whole blood (HWB) with IC₅₀ of 51 nM and 197 nM, respectively^[1].
Ritlecitinib tosylate inhibits the phosphorylation of STAT proteins mediated by IL-2 (STAT5), IL-4 (STAT6), IL-7 (STAT5), IL-15 (STAT5), and IL-21 (STAT3) at concentrations of 244 nM, 340 nM, 407 nM, 266 nM, and 355 nM (IC₅₀), respectively^[2].
Ritlecitinib tosylate (30 nM, 167 nM; 5 days, 6 days) inhibits cell differentiation in Th1 and Th17 cell differentiation inhibition experiments for 5 days under Th1 conditions and 6 days under Th17 conditions, respectively^[2].

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

Western Blot Analysis^[1]

Cell Line:

Mouse splenocytes, human whole blood lymphocytes (HWB)
Concentration:

33.1 nM, 244 nM, 340 nM, 407 nM, 266 nM, 355 nM
Incubation Time:

1 hour (pre-treatment with Ritlecitinib tosylate) + 15-20 minutes (cytokine stimulation)
Result:

In mouse splenocytes, 33.1 nM inhibited JAK3 kinase activity, while 244 nM, 340 nM, 407 nM, and 266 nM inhibited STAT5 phosphorylation induced by IL-2, IL-4, IL-7, and IL-15 respectively. In human whole blood lymphocytes, 355 nM inhibited IL-21-induced STAT3 phosphorylation.

In Vivo

Ritlecitinib (3, 10, 30 mg/kg; oral; once daily; 7 days) tosylate reduces joint swelling and improves disease severity in a dose-dependent manner in the Sprague-Dawley rat adjuvant-induced arthritis (AIA) model^[2].
Ritlecitinib (30, 100 mg/kg (reversal); 20, 60 mg/kg (prevention); oral; once daily) tosylate reduces disease severity in the mouse experimental autoimmune encephalomyelitis (EAE) model^[2].
Ritlecitinib (30 mg/kg; oral; once daily; 4 weeks) tosylate can prevent the occurrence of alopecia areata in the C3H/HeJ mouse skin transplantation alopecia areata prevention model; Ritlecitinib (30 mg/kg; oral; once daily; 12 weeks) tosylate can reverse the symptoms of alopecia areata, promote hair regeneration and reduce skin inflammation in the C3H/HeJ mouse alopecia areata model^[3].

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

Animal Model:

C3H/HeJ mice (8-week-old) + alopecia areata model^[3]
Dosage:

30 mg/kg Ritlecitinib
Administration:

Oral via ALZET osmotic pump; once daily; 12 weeks
Result:

Significantly induced hair regrowth, reduced skin-infiltrating CD45⁺ leukocytes, CD44⁺CD62L⁻CD8⁺ T cells, NKG2D⁺CD8⁺ T cells, and IFN-γ⁺CD8⁺ T cells, and decreased Alopecia areata (AA)-associated skin inflammation.

Chemical Information

CAS. Nr. 2192215-81-7
Appearance Solid
Molecular Weight 457.55
Formel C₂₂H₂₇N₅O₄S
Color White to off-white
SMILES

CC(C=C1)=CC=C1S(O)(=O)=O.C=CC(N2[C@@H](C)CC[C@@H](NC3=C4C(NC=C4)=NC=N3)C2)=O
Synonyms

PF-06651600 tosylate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

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

Publications (9)

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Ann Rheum Dis

Augmentation of immunothrombosis as a key mechanism underlying JAK inhibition associated hypercoagulability in rheumatoid arthritis. [Abstract]

2025 Sep 25:S0003-4967(25)04383-3. PMID: 41006174
Blood Adv

Latent membrane proteins from EBV differentially target cellular pathways to accelerate MYC-induced lymphomagenesis. [Abstract]

2022 Jul 26;6(14):4283-4296. PMID: 35605249
Int J Mol Sci

Epstein-Barr Virus BRRF1 Induces Butyrophilin 2A1 in Nasopharyngeal Carcinoma NPC43 Cells via the IL-22/JAK3-STAT3 Pathway. [Abstract]

2024 Dec 15;25(24):13452. PMID: 39769218

Ritlecitinib tosylate purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Dec 15;25(24):13452. [Abstract]

Ritlecitinib (0.5-5 μM) significantly decreased the gene expression level of BTN2A1 in NPC43 cells.

Ritlecitinib tosylate purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Dec 15;25(24):13452. [Abstract]

STAT3, p-STAT3, STAT1, p-STAT1, STAT5, p-STAT5, JNK, and p-JNK protein expression of NPC43 cells by BRRF1 overexpression with or without Ritlecitinib (5 μM) treatment. Representative immunoblots are shown.
Int J Mol Sci

JAK Signaling Is Critically Important in Cytokine-Induced Viral Susceptibility of Keratinocytes. [Abstract]

2023 May 25;24(11):9243. PMID: 37298195
Expert Opin Investig Drugs

Ritlecitinib: an investigational drug for the treatment of moderate to severe alopecia areata. [Abstract]

2021 Dec;30(12):1169-1174. PMID: 34826225
Clin Immunol

Novel janus kinase 3 inhibitor ritlecitinib suppresses T and B cell responses to prevent acute cardiac allograft rejection in mice. [Abstract]

2025 Apr:273:110445. PMID: 39954912
Res Sq

2026 Apr 13.
bioRxiv

2026 Mar 7.
bioRxiv

2023 Aug 17.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 83.33 mg/mL (182.12 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)

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

2.1856 mL

10.9278 mL

21.8555 mL

5 mM

0.4371 mL

2.1856 mL

4.3711 mL

10 mM

0.2186 mL

1.0928 mL

2.1856 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 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)

Verweise

[1]. Thorarensen A, et al. Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2 S, 5 R)-5-((7 H-Pyrrolo [2, 3-d] pyrimidin-4-yl) amino)-2-methylpiperidin-1-yl) prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. Journal of medicinal chemistry, 2017, 60(5): 1971-1993.

[2]. Telliez JB, et al. Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. [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
DMSO	1 mM	2.1856 mL	10.9278 mL	21.8555 mL	54.6388 mL
	5 mM	0.4371 mL	2.1856 mL	4.3711 mL	10.9278 mL
	10 mM	0.2186 mL	1.0928 mL	2.1856 mL	5.4639 mL
	15 mM	0.1457 mL	0.7285 mL	1.4570 mL	3.6426 mL
	20 mM	0.1093 mL	0.5464 mL	1.0928 mL	2.7319 mL
	25 mM	0.0874 mL	0.4371 mL	0.8742 mL	2.1856 mL
	30 mM	0.0729 mL	0.3643 mL	0.7285 mL	1.8213 mL
	40 mM	0.0546 mL	0.2732 mL	0.5464 mL	1.3660 mL
	50 mM	0.0437 mL	0.2186 mL	0.4371 mL	1.0928 mL
	60 mM	0.0364 mL	0.1821 mL	0.3643 mL	0.9106 mL
	80 mM	0.0273 mL	0.1366 mL	0.2732 mL	0.6830 mL
	100 mM	0.0219 mL	0.1093 mL	0.2186 mL	0.5464 mL

Keywords

Ritlecitinib tosylate

9 Cited Publications

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Ritlecitinib tosylate

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Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

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Publications Citing Use of MedChemExpress (MCE) Ritlecitinib tosylate

Alle JAK Isoform-spezifische Produkte anzeigen

Alle Interleukin Related Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ritlecitinib tosylate Related Classifications

HY-100754C Related Classifications