Home JAK/STAT JAK inhibitor Ritlecitinib (PF-06651600) For research use only.

Ritlecitinib (PF-06651600)

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

Ritlecitinib (PF-06651600) Chemical Structure

CAS: 1792180-81-4

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

Purity & Quality Control

Batch: S853801 DMSO] 57 mg/mL] false] Ethanol] 46 mg/mL] false] Water] Insoluble] false Purity: 99.99%
99.99

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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
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 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].
Animal Research Animal Models female Lewis rats (8 to 10 weeks old)
Dosages 80, 15, or 6 mg/kg
Administration via oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04390776 Completed Healthy Participants Pfizer September 28 2020 Phase 1
NCT04266509 Completed Healthy Volunteers Pfizer June 25 2020 Phase 1
NCT04037865 Terminated Renal Impairment Pfizer August 19 2019 Phase 1
NCT04016077 Completed Hepatic Impairment|Healthy Participants Pfizer July 19 2019 Phase 1
NCT04004663 Completed Healthy Volunteers Pfizer July 15 2019 Phase 1

Chemical lnformation & Solubility

Molecular Weight 285.34 Formula

C15H19N5O
CAS No. 1792180-81-4 SDF Download Ritlecitinib (PF-06651600) SDF
Smiles CC1CCC(CN1C(=O)C=C)NC2=NC=NC3=C2C=CN3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (199.76 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 46 mg/mL

Water : Insoluble


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In vivo
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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.

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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.

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