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

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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.
Targets
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:

[1]

  • 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
Formula

C15H19N5O

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

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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