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AU-24118

Chemical Structure : AU-24118

CAS No.:

AU-24118 (AU24118)

Catalog No.: PC-22055Not For Human Use, Lab Use Only.

AU-24118 is a potent, selective, and orally bioavailable degrader of mSWI/SNF ATPases (SMARCA2, SMARCA4) and PBRM1.

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    Biological Activity

    AU-24118 is a potent, selective, and orally bioavailable degrader of mSWI/SNF ATPases (SMARCA2, SMARCA4) and PBRM1.
    AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase.
    AU-24118 selectively degraded SMARCA2, SMARCA4, and PBRM1 in VCaP prostate cancer cells, through the CRBN-based proteasomal degradation machinery.
    AU-24118 induces tumor regression as a single agent, as well as in combination with enzalutamide, in a VCaP CRPC model.
    has increased efficacy compared to AU-15330 in terms of both target degradation efficiency as well as potency in vivo.

    Physicochemical Properties

    M.Wt 632.77
    Formula C37H40N6O4
    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

    3-(4-(1'-(4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)phenyl)-[1,4'-bipiperidin]-4-yl)phenoxy)piperidine-2,6-dione

    References

    1. Tongchen He, et al. bioRxiv. [Preprint]. 2024 Mar 2:2024.02.29.582768.

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