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BI 894999

Chemical Structure : BI 894999

CAS No.: 1610044-98-8

BI 894999 (Amredobresib, BI-894999)

Catalog No.: PC-38620Not For Human Use, Lab Use Only.

BI 894999 is a novel potent, selective BET inhibitor with IC50 of 5 and 41 nM for BRD4-BD1 and BRD4-BD2 bromodomains, respectively.

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    Biological Activity

    BI 894999 (Amredobresib) is a novel potent, selective BET inhibitor with IC50 of 5 and 41 nM for BRD4-BD1 and BRD4-BD2 bromodomains, respectively.
    BI 894999 displays excellent selectivity over other bromodomains.
    BI 894999 decreases S-Phase and increases apoptosis, Volasertib augments and prolongs the decrease of MYC expression caused by BI 894999 treatment in AML cell lines。
    BI 894999 dramatically reduces tumor burden accompanied by eradication of AML cells in mouse bone marrow combined with Volasertib.
    BI 894999 also represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML.

    Physicochemical Properties

    M.Wt 467.581
    Formula C26H29N9
    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

    6-(1-benzyl-6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)-N,3-dimethyl-[1,2,4]triazolo[4,3-a]pyrazin-8-amine

    References

    1. Tontsch-Grunt U, et al. Cancer Lett. 2018 May 1;421:112-120.

    2. Gerlach D, et al. Oncogene. 2018 May;37(20):2687-2701.

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