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PQR514

Chemical Structure : PQR514

CAS No.: 1927857-55-3

PQR514 (PRQ-514)

Catalog No.: PC-73277Not For Human Use, Lab Use Only.

PQR514 is a potent selective pan-PI3K inhibitor with binding Ki of 2.2 and 33 nM for p110α and mTOR, repectively.

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    Biological Activity

    PQR514 is a potent selective pan-PI3K inhibitor with binding Ki of 2.2 and 33 nM for p110α and mTOR, repectively.
    PQR514 inhibits phosphorylated S6 ribosomal protein (pS6, Ser235/236) and phosphorylation PKB Ser473 in A2058 cells with IC50 of 17 and 68 nM, respectively.
    PQR514 displays negligible interference with protein kinase activities at 10 uM in a KINOMEScan panel.
    PQR514 exhibits growth inhibition in vitro across a panel of 66 tumor cells with GI50 of 0.25 uM.
    PQR514 demonstrates significant antitumor activity aginst OVCAR-3 human ovarian cancer xenograft model in BALB/c nude mice.

    Physicochemical Properties

    M.Wt 394.387
    Formula C16H20F2N8O2
    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

    4-(Difluoromethyl)-5-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-2-pyrimidinamine

    References

    1. Chiara Borsari, et al. ACS Med Chem Lett. 2019 Sep 3;10(10):1473-1479.

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