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NK150460

Chemical Structure : NK150460

CAS No.: 709640-62-0

NK150460 (NK 150460;NK-150460)

Catalog No.: PC-60775Not For Human Use, Lab Use Only.

NK150460 is a potent and selective inhibitor of breast cancer cells via activation the aryl hydrocarbon receptor (AhR) pathway.

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    Biological Activity

    NK150460 is a potent and selective inhibitor of breast cancer cells via activation the aryl hydrocarbon receptor (AhR) pathway.
    NK150460 inhibits growth of not only most ER-positive, but also some ER-negative breast cancer cell lines, while never inhibiting growth of non-breast cancer cell lines.
    NK150460 inhibits 17β-estradiol (E2)-dependent transcription without affecting binding of E2 to ER.
    NK150460 does not induce histone H2AX phosphorylation or p53 expression.
    NK150460 is a a novel AhR agonist dependent on AhR/ARNT and cytochrome P450 CYP1A1.

    Physicochemical Properties

    M.Wt 308.304
    Formula C16H15F3N2O
    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

    (5S,7S)-7-methyl-3-(3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydrocinnolin-5-ol

    References

    1. Fukasawa K, et al. Mol Cancer Ther. 2015 Feb;14(2):343-54.

    2. Gilbert J, et al. Mol Pharmacol. 2017 Dec 21. pii: mol.117.109827.

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