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PRC2 EED-IN-1

Chemical Structure : PRC2 EED-IN-1

CAS No.: 2762275-20-5

PRC2 EED-IN-1

Catalog No.: PC-72291Not For Human Use, Lab Use Only.

PRC2 EED-IN-1 is a potent, selective, allosteric, orally bioavailable inhibitor of the EED subunit of histone methyltransferase PRC2 with IC50 of 44 nM (H3K27me3 inhibition).

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    Biological Activity

    PRC2 EED-IN-1 is a potent, selective, allosteric, orally bioavailable inhibitor of the EED subunit of histone methyltransferase PRC2 with IC50 of 44 nM (H3K27me3 inhibition).
    PRC2 EED-IN-1 retains efficacy against EZH2 inhibitor-resistant cell lines (Karpas 44 cell IC50=27 nM), exhibits in vivo efficacy in EZH2-driven tumors in vivo.

    Physicochemical Properties

    M.Wt 394.414
    Formula C19H19FN8O
    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

    N5-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-N8-methyl-N8-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-c]pyrimidine-5,8-diamine

    References

    1. Bagal SK, et al. J Med Chem. 2021 Dec 9;64(23):17146-17183.

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