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DS-9300

Chemical Structure : DS-9300

CAS No.: 2259641-46-6

DS-9300 (DS9300)

Catalog No.: PC-49530Not For Human Use, Lab Use Only.

DS-9300 (DS9300) is a highly potent, selective and orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with IC50 of 28 nM, inhibits cellular acetylation of histone H3K27 (H3K27Ac) with IC50 of 54 nM.

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    Biological Activity

    DS-9300 (DS9300) is a highly potent, selective and orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with IC50 of 28 nM, inhibits cellular acetylation of histone H3K27 (H3K27Ac) with IC50 of 54 nM.
    DS-9300 inhibits VCaP cell growth with GI50 of 0.6 nM, and DS-9300 (3 mg/kg, once daily, oral) demonstrated potent antitumor effects in a castrated VCaP xenograft mouse model without significant body weight loss.

    Physicochemical Properties

    M.Wt 501.510
    Formula C25H26F3N5O3
    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

    (2R,4R)-1-(4,4-difluoro-1-(4-methoxyphenyl)cyclohexane-1-carbonyl)-4-fluoro-N-(1H-pyrazolo[4,3-b]pyridin-5-yl)pyrrolidine-2-carboxamide

    References

    1. Kanada R, et al. J Med Chem. 2022 Dec 26. doi: 10.1021/acs.jmedchem.2c01641.

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