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QA-68-ZU81

Chemical Structure : QA-68-ZU81

CAS No.:

QA-68-ZU81 (BRD9 degrader QA-68)

Catalog No.: PC-49151Not For Human Use, Lab Use Only.

QA-68-ZU81 (QA-68) is a EA-89-based BRD9 degrader that incorporates the EA-89 warhead into a cereblon (CRBN)-targeting proteolysis-targeting chimera (PROTAC).

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    Biological Activity

    QA-68-ZU81 (QA-68) is a EA-89-based BRD9 degrader that incorporates the EA-89 warhead into a cereblon (CRBN)-targeting proteolysis-targeting chimera (PROTAC).
    QA-68 causes concentration-dependent inhibition of proliferation of MV4-11, SKM-1 and Kasumi-1-luc+ cells (IC50=1-10 nM for MV4;11 and SKM-1, and IC50=10-100 nM for Kasumi-1-luc +), shows less sensitivity HEL, KO52 and THP-1.
    QA-68 more effectively inhibits SKM-1 cell cycle progression than EA-89, affects cell growth, differentiation, and colony formation in AML cells.

    Physicochemical Properties

    M.Wt 1169.427
    Formula C61H72N10O10S2
    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

    N-(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)-7-(1-((1-(4-(4-(4-(4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)but-3-yn-1-yl)piperazine-1-carbonyl)piperazin-1-yl)-4-oxobutanoyl)piperidin-4-yl)methyl)-3-methyl-1H-indol-5-yl)-4-oxo-5-propyl-4,5-dihydrothieno[3,2-c]pyridine-2-carboxamide

    References

    1. Ellen Weisberg, et al. Blood Cancer J. 2022 Jul 19;12(7):110.

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