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    DRUG:

    VRN08

    i
    Other names: VRN08, VRN-08, VRN081569, VRN-081569
    Company:
    Voronoi
    Drug class:
    TTK inhibitor
    Related drugs:
    3years
    [VIRTUAL] VRN08, a Selective Mps1 Kinase Inhibitor Induces Mitotic Catastrophe and Apoptosis Efficiently in Advanced Cancers Including Rb1-Deficient (AACR 2021)
    Especially we confirmed that VRN081569 induces caspase 3/7 activity faster in Rb1-negative cells (~50-fold EC50 of caspase 3/7 activity compared to Rb1-positive cells), and cell cycle analysis has shown that our compound induces a dose-dependent dysregulation of mitosis, resulting in a decrease in the frequency of the G0/G1 phase, and also induces aneuploidy and apoptosis. Finally, we confirmed a combination effects with anti-microtubule agents BCL-2 inhibitor and PARP-1 inhibitor, suggesting that modulation of two different cellular processes may overcome the lack of single agent activity for TNBC.
    Late-breaking abstract
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    RB1 (RB Transcriptional Corepressor 1) • CASP3 (Caspase 3) • CASP7 (Caspase 7)
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    RB1 positive • RB1 negative
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    VRN08