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CRBN(BRAF)-24

Chemical Structure : CRBN(BRAF)-24

CAS No.:

CRBN(BRAF)-24 (BRAF V600E PROTAC)

Catalog No.: PC-38718Not For Human Use, Lab Use Only.

CRBN(BRAF)-24 is a potent small molecule degrader against oncogenic BRAF V600E protein, potently degrades BRAFV600E in a ubiquitin–proteasome system (UPS)-dependent manner and inhibits the proliferation of BRAFV600E-driven cancer cells.

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    Biological Activity

    CRBN(BRAF)-24 is a potent small molecule degrader against oncogenic BRAF V600E protein, potently degrades BRAFV600E in a ubiquitin–proteasome system (UPS)-dependent manner and inhibits the proliferation of BRAFV600E-driven cancer cells.
    CRBN(BRAF)-24 showed more potent and sustained suppression of MAPK signaling than a BRAFV600E inhibitor, PLX-8394, in BRAFV600E-driven cancer cells.
    CRBN(BRAF)-24 induced neither BRAFWT degradation nor paradoxical activation of the MAPK pathway in BRAF wild-type cells.

    Physicochemical Properties

    M.Wt 1111.168
    Formula C53H57F3N12O10S
    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

    (3R)-N-(3-(5-(2-(4-(4-(1-(3-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)propanoyl)piperidin-4-yl)butanoyl)piperazin-1-yl)pyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)-3-fluoropyrrolidine-1-sulfonamide

    References

    1. Nobumichi Ohoka, et al. Cancer Sci. 2022 May 17. doi: 10.1111/cas.15401.

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