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    DRUG:

    CHIR-124

    i
    Other names: CHIR-124, CHIR124, CHIR 124
    Company:
    Novartis
    Drug class:
    Chk1 inhibitor
    Related drugs:
    4ms
    A high-throughput approach to identify BRCA1-downregulating compounds to enhance PARP inhibitor sensitivity. (PubMed, iScience)
    Three compounds, N-acetyl-N-acetoxy chlorobenzenesulfonamide (NANAC), A-443654, and CHIR-124, were validated to reduce BRCA1 protein levels and sensitize breast cancer cells to the toxic effects of olaparib. These results suggest that BRCA1-HiBiT reporter cells hold promise in developing agents to improve the clinical utility of PARPi.
    Journal • BRCA Biomarker • PARP Biomarker
    |
    BRCA1 (Breast cancer 1, early onset)
    |
    Lynparza (olaparib) • CHIR-124 • A 443654