Home JAK/STAT JAK inhibitor Ropsacitinib (PF-06826647)

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Ropsacitinib (PF-06826647) JAK inhibitor

Cat.No.S9676

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. It also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively, and is used in the treatment of psoriasis (PSO).
Ropsacitinib (PF-06826647) JAK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 383.41

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Quality Control

Batch: Purity: 99.48%
99.48

Solubility

In vitro
Batch:

DMSO : 77 mg/mL (200.82 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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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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Chemical Information, Storage & Stability

Molecular Weight 383.41 Formula

C20H17N9

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2127109-84-4 -- Storage of Stock Solutions

Synonyms Tyk2-IN-8, compound 10 Smiles CN1C=C(C=N1)C2=CN3C(=CC=N3)C(=N2)C4=CN(N=C4)C5(CC(C5)C#N)CC#N

Mechanism of Action

Targets/IC50/Ki
TYK2
(Cell-free assay)
17 nM
JAK2
(Cell-free assay)
74 nM
JAK1
(Cell-free assay)
383 nM
In vitro

Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 22) 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. It also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively.
In vivo

Ropsacitinib (PF-06826647) is a potent TYK2 inhibitor binding to the JH1 domain. It inhibits ear swelling in the induced skin inflammation model.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04134715 Completed
Healthy
Pfizer
 October 23 2019 Phase 1

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