Home JAK/STAT JAK inhibitor Ropsacitinib (PF-06826647) For research use only.

Ropsacitinib (PF-06826647)

Synonyms: Tyk2-IN-8, compound 10

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

Ropsacitinib (PF-06826647) Chemical Structure

CAS No. 2127109-84-4

Purity & Quality Control

Ropsacitinib (PF-06826647) Related Products

Signaling Pathway

JAK Signaling Pathways

JAK Signaling Pathway

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 vitro
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
In vivo

PF-06826647 is a potent TYK2 inhibitor binding to the JH1 domain. PF-06826647 inhibits ear swelling in the induced skin inflammation model.[2]
Animal Research Animal Models TYK2 Val980Ile mice
Dosages 30 mg/kg, 10 mg/kg, 3 mg/kg, 1 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04134715 Completed
Healthy
Pfizer
 October 23 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 383.41 Formula

C20H17N9
CAS No. 2127109-84-4 SDF --
Smiles CN1C=C(C=N1)C2=CN3C(=CC=N3)C(=N2)C4=CN(N=C4)C5(CC(C5)C#N)CC#N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 77 mg/mL ( (200.82 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

Handling Instructions

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