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CRCM5484

Chemical Structure : CRCM5484

CAS No.: 3022975-51-2

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CRCM5484 (CRCM-5484)

Catalog No.: PC-72866Not For Human Use, Lab Use Only.

CRCM5484 is a potent, BET BDII-selective inhibitor with IC50 of 130/20/71 nM for BRD4-BD2/BRD3-BD2/BRD2-BD2, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    CRCM5484 is a potent, BET BDII-selective inhibitor with IC50 of 130/20/71 nM for BRD4-BD2/BRD3-BD2/BRD2-BD2, respectively.
    CRCM5484 displays 475-fold selectivity over its first bromodomain (BRD3-BD2 vs BRD3-BD1).
    CRCM5484 demonstrates very low activity in various cell-based assays.
    CRCM5484 modulates the anti-leukemic activity in combination with various FDA-approved and/or in-development drugs in a cell- and context-dependent differential manner.

    Physicochemical Properties

    M.Wt 509.599
    Formula C24H23N5O4S2
    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

    2-((7-acetyl-3-(furan-2-ylmethyl)-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl)thio)-N-(2-methylpyridin-3-yl)acetamide

    References

    1. Kendall Carrasco, et al. J Med Chem. DOI: 10.1021/acs.jmedchem.1c02168

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