Ritlecitinib (Synonyms: PF-06651600)

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

Cat. No.: HY-100754 Purity: 99.43%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

Ritlecitinib (PF-06651600) is an orally active and selective JAK3 inhibitor with an IC₅₀ of 33.1 nM.

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

Ritlecitinib Chemical Structure

CAS No. : 1792180-81-4

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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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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

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JAK1 JAK2 JAK3 Tyk2 JAK

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Ritlecitinib (PF-06651600) is an orally active and selective JAK3 inhibitor with an IC₅₀ of 33.1 nM^[1].

IC₅₀ & Target^[1]

JAK3

33.1 nM (IC₅₀)

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 is a potent JAK3-selective inhibitor which can inhibit the JAK3 kinase activity with an IC₅₀ of 33.1 nM but without activity (IC₅₀>10 000 nM) against JAK1, JAK2, and TYK2. Ritlecitinib inhibits the phosphorylation of STAT5 elicited by IL-2, IL-4, IL-7, and IL-15 with IC₅₀ values of 244, 340, 407, and 266 nM, respectively. Ritlecitinib also inhibits the phosphorylation of STAT3 elicited by IL-21 with an IC₅₀ of 355 nM. Functional assessment in T-cell differentiation assays demonstrate that Ritlecitinib suppresses Th1 and Th17 differentiation as measured by IFNγ, after 5 days under Th1 conditions, and IL-17 production, after 6 days under Th17 conditions, with IC₅₀ values of 30 nM and 167 nM, respectively. Ritlecitinib also suppresses Th1 and Th17 function as measured by the inhibition of IFNγ production (IC₅₀=48 nM) and IL-17 production (IC₅₀=269 nM) in cells that have been previously differentiated and rested before being treated with PF-06651600^[1].

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

In Vivo

In the rat adjuvant-induced arthritis (AIA) model, Ritlecitinib reduces paw swelling with an unbound EC₅₀ of 169 nM. Similarly, Ritlecitinib significantly reduces disease severity in the experimental autoimmune encephalomyelitis (EAE) mouse model when dosed either therapeutically at 30 or 100 mg/kg or prophylactically at 20 and 60 mg/kg. The efficacy of Ritlecitinib in these two rodent models of inflammatory and autoimmune diseases illustrates that JAK3-selective inhibition can be sufficient to have disease modifying effects in human diseases^[1].

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

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 (281 KB) SDS (393 KB)

COA (253 KB) HNMR (226 KB) NP-HPLC (103 KB) LCMS (110 KB)

Handling Instructions (2659 KB)

References

[1]. 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]

Cell Assay ^[1]	To study the effect of PF-06651600 on Th17 cells post differentiation, skewed Th17 cells are washed, rested with medium for overnight and resuspended in medium containing the same concentrations of cytokines as during skewing but without anti-CD3 or anti-CD28 antibodies, in the presence of PF-06651600 at 10 different concentrations for 2 additional days. On Day 9, supernatant is harvested from each well and IL-17A is determined^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	The effect of JAK3 inhibition by PF-06651600 is evaluated in vivo using a therapeutic dosing paradigm in a rat adjuvant-induced arthritis. When individual hind paw volume measurements indicate an increase of 0.2 mL (or greater) in a single hind paw, animals are randomly assigned to a treatment group. Daily treatment with PF-06651600 is administered via oral gavage. Treatment groups for Experiment 1 are: 80, 15, or 6 mg/kg of PF-06651600 or vehicle (2% Tween 80/0.5% methylcellulose/deionized water). Treatment groups for Experiment 2 are: 30, 10, and 3 mg/kg of PF-06651600 or vehicle (0.5% methylcellulose/de-ionized water/1 mEQ hydrochloric acid). Treatment groups for Experiment 3 are: 10, 1, 0.3 and 0.1 mg/kg of PF-06651600 or vehicle (0.5% methylcellulose/de-ionized water/1 mEQ hydrochloric acid). Treatment continues for 7 days^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. 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 06651600JAKJanus kinaseInhibitorinhibitorinhibit

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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:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Ritlecitinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Ritlecitinib Related Classifications

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