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    DRUG:

    Compound 6a

    i
    Other names: Compound 6a
    Company:
    Binzhou Medical University, Sun Yat-sen University
    Drug class:
    EGFR inhibitor
    Related drugs:
    2years
    Novel third-generation pyrimidines-based EGFR tyrosine kinase inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. (PubMed, Bioorg Chem)
    Among them, Compound 6a showed good inhibitory activity against EGFR mutant cells with an IC value of 0.0022 ± 0.001 μM and was approximately 1730-fold less potent against EGFR WT cells (IC: 4.499 ± 0.057 μM)...Additionally, in vivo studies confirmed that 6a suppressed tumor growth in an H1975 xenograft model (25 mg/kg/d, TGI: 90.24%). Overall, these results suggest that 6a could be a promising lead compound for overcoming the clinical EGFR T790M resistance of patients with non-small-cell lung cancers (NSCLCs).
    Journal
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR T790M • EGFR wild-type • EGFR H1975
    |
    Compound 6a