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Culmerciclib

Chemical Structure : Culmerciclib

CAS No.: 2004705-28-4

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Culmerciclib (TQB3616, TQB 3616)

Catalog No.: PC-49131Not For Human Use, Lab Use Only.

TQB3616 (Culmerciclib) is a potent, selective inhibitor of CDK4/6, shows remarkable inhibitory effect on hormone receptor-positive breast cancer cells.

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

    Biological Activity

    TQB3616 (Culmerciclib) is a potent, selective inhibitor of CDK4/6, shows remarkable inhibitory effect on hormone receptor-positive breast cancer cells.
    TQB3616 potently inhibits tumor cell proliferation for T47D cells (IC50=82.4 nM) and MCF-7 cells (IC50=115.5 nM).
    TQB3616 shows better inhibitory activity in the HER2-positive /HR-positive breast cancer cells than abemaciclib.
    TQB3616 (1.5 uM) reduces colony formation of T47D and BT474 cells, inhibits the abnormal activation of phosphorylated Cyclin D protein.
    TQB3616 not only induced G1 stalling, leading to a profound reduction in the level of RB protein phosphorylated at Ser807/811, but also showed enhanced tumor killing effects by promoting cell apoptosis.
    TQB3616 showed more potent antitumor activity than abemaciclib in an in vitro breast cancer xenograft model.

    Physicochemical Properties

    M.Wt 446.534
    Formula C24H27FN8
    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-fluoro-4-[2-methyl-3-(propan-2-yl)-2H-indazol-5-yl]-N-[5-(piperazin-1-yl)pyridin-2-yl]pyrimidin-2-amine

    References

    1. Patent WO2021259203 A1 2021-12-30.

    2. Patent WO2016141881 A1 2016-09-15.

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