國家衛生研究院 NHRI:Item 3990099045/6175
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    題名: BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML
    作者: Lin, WH;Jiaang, WT;Chen, CW;Yen, KJ;Hsieh, SY;Yen, SC;Chen, CP;Chang, KY;Chang, CY;Chang, TY;Huang, YL;Yeh, TK;Chao, YS;Chen, CT;Hsu, JT
    貢獻者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Background:Activating mutations of Fms-like tyrosine kinase 3 (FLT3) constitute a major driver in the pathogenesis of acute myeloid leukaemia (AML). Hence, pharmacological inhibitors of FLT3 are of therapeutic interest for AML.Methods:The effects of inhibition of FLT3 activity by a novel potent FLT3 inhibitor, BPR1J-097, were investigated using in vitro and in vivo assays.Results:The 50% inhibitory concentration (IC(50)) of BPR1J-097 required to inhibit FLT3 kinase activity ranged from 1 to 10 nM, and the 50% growth inhibition concentrations (GC(50)s) were 21+/-7 and 46+/-14 nM for MOLM-13 and MV4-11 cells, respectively. BPR1J-097 inhibited FLT3/signal transducer and activator of transcription 5 phosphorylation and triggered apoptosis in FLT3-driven AML cells. BPR1J-097 also showed favourable pharmacokinetic property and pronounced dose-dependent tumour growth inhibition and regression in FLT3-driven AML murine xenograft models.Conclusion:These results indicate that BPR1J-097 is a novel small molecule FLT-3 inhibitor with promising in vivo anti-tumour activities and suggest that BPR1J-097 may be further developed in preclinical and clinical studies as therapeutics in AML treatments.
    日期: 2012-01
    關聯: British Journal of Cancer. 2012 Jan;106(3):475-481.
    Link to: http://dx.doi.org/10.1038/bjc.2011.564
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0007-0920&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000300302300008
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84856409052
    顯示於類別:[徐祖安] 期刊論文
    [陳炯東] 期刊論文
    [葉燈光] 期刊論文
    [蔣維棠] 期刊論文
    [趙宇生(2002-2013)] 期刊論文

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