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PI3Kβ/δ inhibitor 20a

Chemical Structure : PI3Kβ/δ inhibitor 20a

CAS No.: 1842380-77-1

PI3Kβ/δ inhibitor 20a (PI3K-IN-6)

Catalog No.: PC-61135Not For Human Use, Lab Use Only.

PI3Kβ/δ inhibitor 20a is a potent, highly selective PI3Kβ/δ inhibitor with IC50 of 7.8/5.3 nM respectively, with liitle to no activity on PI3Kα/γ (IC50=850/>10,000 nM).

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

    Biological Activity

    PI3Kβ/δ inhibitor 20a is a potent, highly selective PI3Kβ/δ inhibitor with IC50 of 7.8/5.3 nM respectively, with liitle to no activity on PI3Kα/γ (IC50=850/>10,000 nM).
    PI3Kβ/δ inhibitor 20a inhibits the phosphorylation of AKT1 Ser473 in PI3K-dependent cell lines with EC50 of 3.4-7.3 nM, inhibits AKT Ser473 phosphorylation and cell viability of LNCaP tumor cells with EC50 of 7.3 nM and GI50 of 38 nM.
    PI3Kβ/δ inhibitor 20a demonstrates efficacy in human PTEN-deficient LNCaP prostate carcinoma xenograft tumor model.

    Physicochemical Properties

    M.Wt 450.259
    Formula C17H14Cl2FN9O
    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

    (S)-8-chloro-2-(1-((2,6-diamino-5-chloropyrimidin-4-yl)amino)ethyl)-6-fluoro-3-(1H-pyrazol-3-yl)quinazolin-4(3H)-one

    References

    1. Perreault S, et al. J Med Chem. 2017 Feb 23;60(4):1555-1567.

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