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CBPD-409

Chemical Structure : CBPD-409

CAS No.: 3037549-86-0

CBPD-409 (CBPD409)

Catalog No.: PC-22054Not For Human Use, Lab Use Only.

CBPD-409 (CBPD409) is a highly potent, selective, and orally bioavailable CBP/p300 degrader with DC50 0.2-0.4 nM in VCaP, LNCaP, and 22Rv1 AR+ prostate cancer cell lines.

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

    Biological Activity

    CBPD-409 (CBPD409) is a highly potent, selective, and orally bioavailable CBP/p300 degrader with DC50 0.2-0.4 nM in VCaP, LNCaP, and 22Rv1 AR+ prostate cancer cell lines.
    CBPD-409displays strong antiproliferative effects with IC50 1.2-2.0 nM in the VCaP, LNCaP, and 22Rv1 AR+ prostate cancer cell lines.
    CBPD-409 at 1 mg/kg achieves >95% depletion of CBP/p300 proteins in the VCaP tumor tissue.
    CBPD-409 exhibits strong tumor growth inhibition and is much more potent and efficacious thanCBP/p300 inhibitors CCS1477 and GNE-049 and the AR antagonist Enzalutamide.

    Physicochemical Properties

    M.Wt 862.98
    Formula C46H52F2N10O5
    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

    5-(4-(((1r,4r)-4-(5-Acetyl-3-(7-(difluoromethyl)-6-(1-methyl-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)cyclohexyl)methyl)piperazin-1-yl)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

    References

    1. Zhixiang Chen, et al. J Med Chem. 2024 Mar 26.

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