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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-OM-153
OM-153

Chemical Structure : OM-153

CAS No.: 2406278-81-5

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OM-153 (OM153)

货号: PC-38617Not For Human Use, Lab Use Only.

OM-153 (OM153) is a potent, selective tankyrase 1 and 2 (TNKS1/2) inhibitor with IC50 of 13 nM and 2 nM, respectively, specifically inhibits WNT/β-catenin signaling with IC50 of 0.63 nM, does not inhibit PARP1.

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

    生物&药学活性

    OM-153 (OM153) is a potent, selective tankyrase 1 and 2 (TNKS1/2) inhibitor with IC50 of 13 nM and 2 nM, respectively, specifically inhibits WNT/β-catenin signaling with IC50 of 0.63 nM, does not inhibit PARP1.
    OM-153 inhibits cell growth in the APC-mutated colon carcinoma cell line COLO 320DM with GI50 of 10 nM.
    OM-153 inhibits WNT/β-catenin, YAP, and MYC signaling and shows an antiproliferative effect in human cancer cell lines.
    OM-153 induces formation of β-catenin and AXIN1-containing puncta and reduces nuclear β-catenin in COLO 320DM cells.
    OM-153 (i.v., 0.4 or 2 mg/kg) or oral (p.o., 10 or 100 mg/kg) inhibits WNT/β-catenin signaling and shows antitumor effect in a human colon carcinoma xenograft model.

    物理化学性质&存储条件

    分子量 509.545
    分子式 C28H24FN7O2
    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

    5-Quinoxalinecarboxamide, N-[trans-3-[5-(5-ethoxy-2-pyridinyl)-4-(2-fluorophenyl)-4H-1,2,4-triazol-3-yl]cyclobutyl]-

    参考文献

    1. Ruben G G Leenders, et al. J Med Chem. 2021 Dec 23;64(24):17936-17949.

    2. Shoshy A. Brinch, et al. Cancer Research Communications (2022) 2 (4): 233–245.

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