2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Immunology/Inflammation
  3. JAK Interleukin Related STAT
  4. Ritlecitinib tosylate

Ritlecitinib tosylate  (Synonyms: PF-06651600 tosylate)

Cat. No.: HY-100754C Purity: 99.77%
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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).

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

Ritlecitinib tosylate Chemical Structure

Ritlecitinib tosylate Chemical Structure

CAS No. : 2192215-81-7

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Ritlecitinib tosylate:

Ritlecitinib tosylate Related Antibodies

Top Publications Citing Use of Products

View All JAK Isoform Specific Products:

View All Isoforms
JAK1 JAK2 JAK3 Tyk2 JAK

View All Interleukin Related Isoform Specific Products:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

View All STAT Isoform Specific Products:

View All Isoforms
STAT3 STAT5 STAT6 STAT1

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Description

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)[1][2][3].

IC50 & Target

JAK3

33.1 nM (IC50)

IL-2

 

IL-4

 

IL7R

 

IL-15

 

STAT3

 

STAT5

 

STAT6

 

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.

Ritlecitinib tosylate Related Antibodies

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.
Molecular Weight

457.55

Formula

C22H27N5O4S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°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 : 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1856 mL 10.9278 mL 21.8555 mL
5 mM 0.4371 mL 2.1856 mL 4.3711 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.

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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.

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
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Ritlecitinib 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:

Ritlecitinib2192215-81-7PF-06651600PF06651600PF 06651600JAKInterleukin RelatedSTATJanus kinaseILInhibitorinhibitorinhibit

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