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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-AZ1366
AZ1366

Chemical Structure : AZ1366

CAS No.: 1645286-58-3

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AZ1366 (AZ-1366)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 416.48
    分子式 C24H24N4O3
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    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

    参考文献

    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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