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GSK143

Chemical Structure : GSK143

CAS No.: 1240390-27-5

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GSK143 (GSK-143;GSK 143)

Catalog No.: PC-63376Not For Human Use, Lab Use Only.

GSK143 is a highly potent, selective, orally efficacious Syk inhibitor with pIC50 of 7.5, >600-fold selective over ZAP-70.

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

    Biological Activity

    GSK143 is a highly potent, selective, orally efficacious Syk inhibitor with pIC50 of 7.5, >600-fold selective over ZAP-70.
    GSK143 inhibits anti-IgM induced Erk1/2 phosphorylation in Ramos cells with pIC50 of 7.1, and anti-IgM induced CD69 surface expression in primary B cells with pIC50 of 6.6.
    GSK143 shows good efficacy in the rat Arthus model.

    Physicochemical Properties

    M.Wt 342.396
    Formula C17H22N6O2
    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

    2-(((3R,4R)-3-aminotetrahydro-2H-pyran-4-yl)amino)-4-(p-tolylamino)pyrimidine-5-carboxamide

    References

    1. Liddle J, et al. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6188-94.

    2. van Bree SH, et al. Gut. 2013 Nov;62(11):1581-90.

    3. Salehi S, et al. PLoS One. 2017 Jan 20;12(1):e0163614.

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