Ritlecitinib (PF-06651600)

Catalog No.S8538

For research use only.

Ritlecitinib (PF-06651600) is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2.

Ritlecitinib (PF-06651600) Chemical Structure

CAS No. 1792180-81-4

Selleck's Ritlecitinib (PF-06651600) has been cited by 2 Publications

Purity & Quality Control

Choose Selective JAK Inhibitors

Other JAK Products

Biological Activity

Description Ritlecitinib (PF-06651600) is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2.
JAK3 [1]
(Cell-free assay)
33.1 nM
In vitro

PF-06651600, a newly discovered potent JAK3-selective inhibitor, is highly efficacious at inhibiting γc cytokine signaling, which is dependent on both JAK1 and JAK3. In vitro, it inhibits Th1 and Th17 cell differentiation and function. In total lymphocytes in human whole blood, PF-06651600 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, and it inhibits the phosphorylation of STAT3 elicited by IL-21 with an IC50 of 355 nM[1].

In vivo In vivo, PF-06651600 reduces disease pathology in rat adjuvant-induced arthritis as well as in mouse experimental autoimmune encephalomyelitis models. PF-06651600 has suitable pharmacokinetics and pharmacodynamics properties for preclinical and clinical evaluations. Human pharmacokinetics of PF-06651600 are predicted to show approximate values of blood clearance of 5.6 mL/min/kg, a steady state volume of distribution of 1.3 L/kg, oral bioavailability of 90%, and a systemic half-life of 2 h[1].

Protocol (from reference)

Animal Research:


  • Animal Models: female Lewis rats (8 to 10 weeks old)
  • Dosages: 80, 15, or 6 mg/kg
  • Administration: via oral gavage

Chemical Information

Molecular Weight 285.34


CAS No. 1792180-81-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CCC(CN1C(=O)C=C)NC2=NC=NC3=C2C=CN3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O

Calculation results:

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 ddH2O, 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04390776 Completed Drug: PF-06651600 Healthy Participants Pfizer September 28 2020 Phase 1
NCT04266509 Completed Drug: PF-06651600|Drug: Rifampin Healthy Volunteers Pfizer June 25 2020 Phase 1
NCT04037865 Terminated Drug: PF-06651600 Renal Impairment Pfizer August 19 2019 Phase 1
NCT04016077 Completed Drug: PF-06651600 30 mg Hepatic Impairment|Healthy Participants Pfizer July 19 2019 Phase 1
NCT04004663 Completed Drug: PF-06651600 Healthy Volunteers Pfizer July 15 2019 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Ritlecitinib (PF-06651600) | Ritlecitinib (PF-06651600) supplier | purchase Ritlecitinib (PF-06651600) | Ritlecitinib (PF-06651600) cost | Ritlecitinib (PF-06651600) manufacturer | order Ritlecitinib (PF-06651600) | Ritlecitinib (PF-06651600) distributor