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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-MCI-030
MCI-030

Chemical Structure : MCI-030

CAS No.: 2700025-84-7

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MCI-030 (ADT 061)

货号: PC-49420Not For Human Use, Lab Use Only.

MCI-030 (ADT 061) is a potent, selective PDE10 inhibitor, inhibits recombinant PDE10 using cGMP as a substrate with IC50 of 0.3 uM.

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

    生物&药学活性

    MCI-030 (ADT 061) is a potent, selective PDE10 inhibitor, inhibits recombinant PDE10 using cGMP as a substrate with IC50 of 0.3 uM.
    MCI-030 (ADT 061) is specific for PDE10 and shows no appreciably affecting the activity of all other PDE isozymes.
    MCI-030 (ADT 061) completely lacked COX-1 or COX-2 inhibitory activity at concentrations up to 50 μM.
    MCI-030 (ADT 061) potently inhibited the growth of colon cancer cell lines, HCT116, HT-29, and SW480, with IC50 values of 0.31, 0.33, and 0.37 μM, respectively, but did not appreciably affect the growth of normal colon mucosal (NCM460) cells up to 50 μM.
    ADT 061 activates cGMP/PKG signaling and suppresses oncogenic β-catenin TCF/LEF transcriptional activity in HT-29 colon cancer cells, blocks Wnt-induced nuclear translocation of β-catenin.
    MCI-030 (ADT 061) decreased ovarian cancer cell growth and induced cell cycle arrest and apoptosis in vitro.
    MCI-030 (ADT 061) inhibited colon adenomas in the Apc+/Min-FCCC mouse model, orally active.

    物理化学性质&存储条件

    分子量 472.541
    分子式 C28H28N2O5
    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

    (Z)-2-(5-methoxy-2-methyl-1-(3,4,5-trimethoxybenzylidene)-1H-inden-3-yl)-N-(pyridin-3-yl)acetamide

    参考文献

    1. Kevin J Lee, et al. Cancer Prev Res (Phila). 2021 Nov;14(11):995-1008.

    2. Borneman RM, et al. J Ovarian Res. 2022 Nov 2;15(1):120.

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