A TYK2 inhibitor
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PF-06826647

Item No. 37577

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
trans-3-cyano-1-[4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl]-1H-pyrazol-1-yl]-cyclobutaneacetonitrile
CAS Number
2127109-84-4
Synonyms
  • Ropsacitinib
  • TYK2-IN-8
  • TYK2 Inhibitor 8
Molecular Formula
C20H17N9
Formula Weight
383.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Methanol: Soluble
SMILES
N#CC[C@]1(N2C=C(C3=NC(C4=CN(C)N=C4)=CN5C3=CC=N5)C=N2)C[C@@H](C1)C#N
InChi Code
InChI=1S/C20H17N9/c1-27-11-15(9-24-27)17-13-28-18(2-5-23-28)19(26-17)16-10-25-29(12-16)20(3-4-21)6-14(7-20)8-22/h2,5,9-14H,3,6-7H2,1H3/t14-,20-
InChi Key
XPLZTJWZDBFWDE-OYOVHJISSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $65

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    5 mg

    $308

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    10 mg

    $585

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    25 mg

    $1,380

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    Product Description

    PF-06826647 is an inhibitor of tyrosine kinase 2 (TYK2; IC50 = 15 nM).1 It is selective for TYK2 over JAK1, JAK2, and JAK3 (IC50s = 383, 74, and >10,000 nM, respectively). PF-06826647 inhibits IL-12-induced phosphorylation of STAT4 in isolated human whole blood (IC50 = 14 nM). In vivo, PF-06826647 (3-30 mg/kg, p.o.) reduces ear edema in a mouse model of skin inflammation induced by the toll-like receptor 7 (TLR7) agonist imiquimod (Item No. 14956).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gerstenberger, B.S., Ambler, C., Arnold, E.P., et al. Discovery of tyrosine kinase 2 (TYK2) inhibitor (PF-06826647) for the treatment of autoimmune diseases. J. Med. Chem. 63(22), 13561-13577 (2020).