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CFT-2718

Chemical Structure : CFT-2718

CAS No.:

CFT-2718 (CFT2718)

Catalog No.: PC-72644Not For Human Use, Lab Use Only.

CFT-2718 (CFT2718) is a benzotriazoloazepine-based BRD4 degrader, rapidly and selectively degrade BRD4 in vitro in a CRBN-dependent manner (DC90=10 nM, 293T cells).

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    Biological Activity

    CFT-2718 (CFT2718) is a benzotriazoloazepine-based BRD4 degrader, rapidly and selectively degrade BRD4 in vitro in a CRBN-dependent manner (DC90=10 nM, 293T cells).
    CFT-2718 is more effective than dinaciclib in controlling cell growth and efficiently reduces BRD4 expression in vitro (H69 cell IC50: 0.02 versus 17.38 nM).
    CFT-2718 is more effective than dinaciclib in control of PDX tumor models in vivo.
    CFT-2718 selectively increased the expression of cleaved PARP, an indicator of apoptosis.
    CFT-2718 caused rapid BRD4 degradation and reduced levels of total and pSer2 RPB1 protein.

    Physicochemical Properties

    M.Wt 811.388
    Formula C45H47ClN10O3
    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

    O=C(C(N(CC1=C2C=CC=C1N[C@H]3CN(CCCCCCN4N=CC(C5=CC=C(N6C(C7(CC7)N=C8C9=CC=C(Cl)C=C9)=NN=C6C)C8=C5)=C4)CC3)C2=O)CC%10)NC%10=O

    References

    1. Sun D, et al. Mol Cancer Ther. 2021 Aug;20(8):1367-1377.

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