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INCB059872

Chemical Structure : INCB059872

CAS No.: 1802909-49-4

INCB059872 (INCB-059872)

Catalog No.: PC-38127Not For Human Use, Lab Use Only.

INCB059872 (INCB-059872, INCB 59872) is a potent, selective, and orally active lysine-specific demethylase 1 (LSD1) inhibitor.

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    Biological Activity

    INCB059872 (INCB-059872, INCB 59872) is a potent, selective, and orally active lysine-specific demethylase 1 (LSD1) inhibitor.
    INCB059872 inhibits the proliferation of a panel of SCLC cell lines with EC50 values ranging from 47 to 377 nM.
    Oral administration of INCB059872 on once daily (QD) and alternative day (QoD) dosing regimens inhibited tumor growth in the NCI-H526 and NCI-H1417 human SCLC xenograft models.
    INCB059872 treatment in these models led to the induction of the FEZ1 and UMODL1 genes relative to vehicle-treated animals, as part of a gene signature in SCLC cell lines that is predictive of LSD1 responsiveness.

    Physicochemical Properties

    M.Wt 386.536
    Formula C23H34N2O3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 1 Month
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    1-((4-(methoxymethyl)-4-((((1R,2S)-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)cyclobutane-1-carboxylic acid

    References

    1. Dai XJ, et al. J Med Chem. 2020 Dec 10;63(23):14197-14215.

    2. Johnston G, et al. Gene. 2020 Aug 20;752:144758.

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