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PF-956980

Chemical Structure : PF-956980

CAS No.: 1262832-74-5

PF-956980 (PF 956980;PF956980)

Catalog No.: PC-60314Not For Human Use, Lab Use Only.

PF-956980 is a potent, highly specific JAK3 inhibitor with IC50 of 4 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    PF-956980 is a potent, highly specific JAK3 inhibitor with IC50 of 4 nM.
    PF-956980 shows only modest inhibition of PKA (6.7 uM) and LCK (10.9 uM) in vitro.
    PF-956980 selectively downregulates JAK2 and JAK3 mRNA, corresponding to changes observed at the protein level.
    PF-956980 shows in vivo activity consistent with in vitro enzyme and whole blood assays (39 ng/ml).
    PF-956980 dose-dependently inhibits the DTH response in mice with EC50 of 5 mg/kg.

    Physicochemical Properties

    M.Wt 342.44
    Formula C18H26N6O
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    {(3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-pyrrolidin-1-yl-methanone

    References

    1. Changelian PS, et al. Blood. 2008 Feb 15;111(4):2155-7.

    2. Steele AJ, et al. Blood. 2010 Nov 25;116(22):4569-77.

    3. Field SD, et al. ACS Chem Biol. 2017 May 19;12(5):1183-1187.

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