Ritlecitinib (Synonyms: PF-06651600)

Name: Ritlecitinib
Brand: MedChemExpress
SKU: HY-100754
Rating: 5.0 (7 reviews)

Cat. No.: HY-100754 Purity: 99.43%: Data Sheet
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Ritlecitinib (PF-06651600) 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 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 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 Chemical Structure

CAS No. : 1792180-81-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Ritlecitinib:

7 Publications Citing Use of MCE Ritlecitinib

Featured Recommendations

•Related Screening Libraries:

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View All JAK Isoform Specific Products:

View All Isoforms

JAK1 JAK2 JAK3 Tyk2 JAK

View All Interleukin Related Isoform Specific Products:

View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

JAK3

33.1 nM (IC₅₀)

IL-4

IL7R

IL-15

STAT3

STAT5

STAT6

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	> 10000 nM Compound: 11; PF-06651600	Antiproliferative activity against mouse BaF3 parent cell measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 parent cell measured after 72 hrs by CCK-8 assay	[PMID: 35860875]
BaF3	IC₅₀	> 10000 nM Compound: 11; PF-06651600	Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK1 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK1 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35860875]
BaF3	IC₅₀	> 10000 nM Compound: 11; PF-06651600	Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK2 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK2 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35860875]
BaF3	IC₅₀	28.1 nM Compound: 11; PF-06651600	Antiproliferative activity against mouse BaF3 cells harboring JAK3 M5111 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring JAK3 M5111 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35860875]
CD4+ve Th	IC₅₀	48 nM Compound: PF-06651600	Inhibition of Th1 cell differentiation in human peripheral blood CD4+ve Th cells assessed as decrease in IFNgamma production measured after 5 days Inhibition of Th1 cell differentiation in human peripheral blood CD4+ve Th cells assessed as decrease in IFNgamma production measured after 5 days	[PMID: 36561076]
U-937	IC₅₀	0.04 μM Compound: 5; PF-06651600	Antiproliferative activity against human U-937 cells harbouring JAK3 M511 mutation assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human U-937 cells harbouring JAK3 M511 mutation assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 35306167]
U-937	IC₅₀	19.5 nM Compound: 11; PF-06651600	Antiproliferative activity against human U-937 cells harboring JAK3 M511135 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human U-937 cells harboring JAK3 M511135 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35860875]

In Vitro

Ritlecitinib 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 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 (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) + 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) 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) reduces disease severity in the mouse experimental autoimmune encephalomyelitis (EAE) model^[2].
Ritlecitinib (30 mg/kg; oral; once daily; 4 weeks) 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) 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
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.

Clinical Trial

Molecular Weight

285.35

Formula

C₁₅H₁₉N₅O

CAS No.

1792180-81-4

Appearance

Solid

Color

White to yellow

SMILES

C=CC(N1[C@@H](C)CC[C@@H](NC2=C3C(NC=C3)=NC=N2)C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (438.06 mM; Need ultrasonic; 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	3.5045 mL	17.5223 mL	35.0446 mL
5 mM	0.7009 mL	3.5045 mL	7.0089 mL
10 mM	0.3504 mL	1.7522 mL	3.5045 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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 (7.29 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 (7.29 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 (7.29 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% Methyl cellulose/0.5% Tween-80 in Saline water
Solubility: 6.67 mg/mL (23.37 mM); Suspended solution; Need ultrasonic

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).

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.

Purity & Documentation

Purity: 99.80% ee.: 99.93%

Select Batch:

Data Sheet (302 KB) SDS (393 KB)

COA (252 KB) HNMR (226 KB) NP-HPLC (103 KB) LCMS (110 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.5045 mL	17.5223 mL	35.0446 mL	87.6114 mL
	5 mM	0.7009 mL	3.5045 mL	7.0089 mL	17.5223 mL
	10 mM	0.3504 mL	1.7522 mL	3.5045 mL	8.7611 mL
	15 mM	0.2336 mL	1.1682 mL	2.3363 mL	5.8408 mL
	20 mM	0.1752 mL	0.8761 mL	1.7522 mL	4.3806 mL
	25 mM	0.1402 mL	0.7009 mL	1.4018 mL	3.5045 mL
	30 mM	0.1168 mL	0.5841 mL	1.1682 mL	2.9204 mL
	40 mM	0.0876 mL	0.4381 mL	0.8761 mL	2.1903 mL
	50 mM	0.0701 mL	0.3504 mL	0.7009 mL	1.7522 mL
	60 mM	0.0584 mL	0.2920 mL	0.5841 mL	1.4602 mL
	80 mM	0.0438 mL	0.2190 mL	0.4381 mL	1.0951 mL
	100 mM	0.0350 mL	0.1752 mL	0.3504 mL	0.8761 mL

Ritlecitinib 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:

Ritlecitinib1792180-81-4PF-06651600PF06651600PF 06651600JAKInterleukin RelatedSTATJanus kinaseILInhibitorinhibitorinhibit

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Ritlecitinib (Synonyms: PF-06651600)

Customer Review

Other Forms of Ritlecitinib:

Ritlecitinib Related Antibodies

7 Publications Citing Use of MCE Ritlecitinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All JAK Isoform Specific Products:

View All Interleukin Related Isoform Specific Products:

View All STAT Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Ritlecitinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Ritlecitinib Related Classifications

Keywords:

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