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AZ1366

Chemical Structure : AZ1366

CAS No.: 1645286-58-3

AZ1366 (AZ-1366)

Catalog No.: PC-49491Not For Human Use, Lab Use Only.

AZ1366 (AZ-1366) is a potent and selective inhibitor of TNSK1/2 with IC50 of 7 nM (TNKS1), also inhibits PARP1 with IC50 of 6 nM, shows Wnt pathway inhibition in DLD-1 cells (IC50<3 nM).

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

    Biological Activity

    AZ1366 (AZ-1366) is a potent and selective inhibitor of TNSK1/2 with IC50 of 7 nM (TNKS1), also inhibits PARP1 with IC50 of 6 nM, shows Wnt pathway inhibition in DLD-1 cells (IC50<3 nM).
    AZ1366 showed qualitatively stronger and longer lasting stabilization of Axin2, TNKS1, and TNKS2 at lower concentrations compared to XAV939 in DLD-1 cells.
    AZ1366 synergistically suppresses NSCLC proliferation when combined with EGFR inhibitor gefitinib, exerts antiproliferative effects through inhibition of the canonical Wnt pathway.
    AZ1366 inhibits basal and Wnt3a-activated β-catenin-dependent transcription in HCCC4006.
    AZ1366 provided increased tumor control and improved survival in mice harboring Wnt-responsive tumors when combined with EGFR inhibitors.

    Physicochemical Properties

    M.Wt 416.48
    Formula C24H24N4O3
    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

    8-(hydroxymethyl)-2-(4-(6-((2-methoxyethyl)amino)-4-methylpyridin-3-yl)phenyl)quinazolin-4(3H)-one

    References

    1. Scarborough HA, et al. Clin Cancer Res. 2017 Mar 15;23(6):1531-1541.

    2. Quackenbush KS, et al. Oncotarget. 2016 May 10;7(19):28273-85.

    3. Johannes JW,et al. ACS medicinal chemistry letters. 2015;6(3):254–59.

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