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    DRUG:

    CCT196969

    i
    Other names: CCT196969
    Company:
    Institute of Cancer Research, The University of Manchester
    Drug class:
    pan-RAF inhibitor, SRC-family kinase (SFK) inhibitor
    Related drugs:
    4ms
    CCT196969 inhibits TNBC by targeting the HDAC5/RXRA/ASNS axis to down-regulate asparagine synthesis. (PubMed, J Exp Clin Cancer Res)
    This study reveals a previously unrecognized anti-TNBC mechanism of CCT196969 through the HDAC5/RXRA/ASNS axis. This provides potential candidate targets for the treatment of TNBC and a theoretical basis for the clinical treatment of TNBC patients with CCT196969.
    Journal
    |
    ASNS (Asparagine synthetase) • HDAC5 (Histone Deacetylase 5) • RXRA (Retinoid X Receptor Alpha)
    |
    CCT196969 • MG132
    3years
    CCT196969 effectively inhibits growth and survival of melanoma brain metastasis cells. (PubMed, PLoS One)
    Furthermore, CCT196969 inhibited viability in two B-Raf Proto-Oncogene (BRAF) inhibitor resistant metastatic melanoma cell lines. Further in vivo studies should be performed to determine the treatment potential of CCT196969 in patients with treatment-naïve and resistant melanoma brain metastasis.
    Journal
    |
    STAT3 (Signal Transducer And Activator Of Transcription 3)
    |
    CCT196969