Ropsacitinib (PF-06826647)

Catalog No.S9676 Synonyms: Tyk2-IN-8, compound 10

For research use only.

Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO).

Ropsacitinib (PF-06826647) Chemical Structure

CAS No. 2127109-84-4

Purity & Quality Control

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Biological Activity

Description Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO).
Targets
TYK2 [1]
(Cell-free assay)
JAK2 [1]
(Cell-free assay)
JAK1 [1]
(Cell-free assay)
17 nM 74 nM 383 nM
In vivo

PF-06826647 is a potent TYK2 inhibitor binding to the JH1 domain. PF-06826647 inhibits ear swelling in the imiquimod-induced skin inflammation model.[2]

Protocol (from reference)

Animal Research:

[2]

  • Animal Models: TYK2 Val980Ile mice
  • Dosages: 30 mg/kg, 10 mg/kg, 3 mg/kg, 1 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 383.41
Formula

C20H17N9

CAS No. 2127109-84-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C=C(C=N1)C2=CN3C(=CC=N3)C(=N2)C4=CN(N=C4)C5(CC(C5)C#N)CC#N

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04134715 Completed Drug: PF-06826647|Drug: Oral Contraceptive (OC) Healthy Pfizer October 23 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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