Ropsacitinib (PF-06826647)

Catalog No.S9676 Batch:S967602

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Technical Data

Formula

C20H17N9
Molecular Weight 383.41 CAS No. 2127109-84-4
Solubility (25°C)* In vitro DMSO 77 mg/mL (200.82 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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

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 Study:

[2]
  • Animal Models

    TYK2 Val980Ile mice

  • Dosages

    30 mg/kg, 10 mg/kg, 3 mg/kg, 1 mg/kg

  • Administration

    Oral gavage

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.