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Dual CARM1-IKZF3 inhibitor 074

Chemical Structure : Dual CARM1-IKZF3 inhibitor 074

CAS No.:

Dual CARM1-IKZF3 inhibitor 074

Catalog No.: PC-24292Not For Human Use, Lab Use Only.

Dual CARM1-IKZF3 inhibitor 074 is a compound composed of the CARM1 inhibitor EZM2302, linked to pomalidomide, increases CRBN-dependent IKZF1, IKZF3, ZFP91, and FGD3 protein degradation, inhibits CRAM1 with IC50 of 2 nM.

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    Biological Activity

    Dual CARM1-IKZF3 inhibitor 074 is a compound composed of the CARM1 inhibitor EZM2302, linked to pomalidomide, increases CRBN-dependent IKZF1, IKZF3, ZFP91, and FGD3 protein degradation, inhibits CRAM1 with IC50 of 2 nM.
    074 more potently suppressed the growth of H929 cells than the combination of EZM2302 and pomalidomide.
    074 074 can potently and selectively kill IMiD-resistant MM cells.
    074 downregulated IKZF3, IKZF1, and MYC more potently than pomalidomide or EZM2302.
    074 was able to override IMiD resistance.

    Physicochemical Properties

    M.Wt 896.44
    Formula C46H54ClN9O8
    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

    4-((6-(2-(2-(2-chloro-5-((R)-2-hydroxy-3-(methylamino)propoxy)phenyl)-6-(3,5-dimethylisoxazol-4-yl)-5-methylpyrimidin-4-yl)-2,7-diazaspiro[3.5]nonan-7-yl)-6-oxohexyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

    References

    1. Ni W, et al. Mol Ther Oncol. 2025 Feb 20;33(1):200952.

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