[Effect of TEB-415, a Derivative of Imatinib, on Multiple Myeloma].

伊马替尼 硼替佐米 化学 IC50型 细胞培养 细胞生长 癌症研究 药理学 分子生物学 多发性骨髓瘤 体外 医学 内科学 生物 生物化学 髓系白血病 遗传学
作者
Xiaomin Wang,Qingdong Xu,Yanan Gao,Juan Gao,Minghao Li,Yanxin Li,Weiping Yuan,Tao Cheng,Yong Li,Yingdai Gao
出处
期刊:PubMed 卷期号:24 (3): 755-9
标识
DOI:10.7534/j.issn.1009-2137.2016.03.022
摘要

To investigate the growth inhibitory effect of Imatinib derivative TEB-415 on various multiple myeloma (MM) cell lines, such as U226, H929, RPMI8226, MM1R and MM1S.TEB-415, a derivative of Imatinib was synthesized by modifying the chemical structure of Imatinib. MM cell lines (U226, H929, RPMI8226, MM1R and MM1S) were treated with TEB-415, Imatini and Bortezomib of various concentrations. Cells were grown for 72 hours and the growth rate was measured by CCK-8 method, cell morphology was observed and the IC50 was calculated.TEB-415 could inhibit H929 and RPMI8226 growth significantly. When the concentration of TEB-415 was <0.1 nmol/L, >50% H929 cells died. The IC50 of Imatinib was 0.123 mol/L while the IC50 of Bortezomib was 0.03 nmol/L. In RPMI8226 cell line, when the concentration of TEB-415 was 11.9 mol/L, more than 50% of cells died. In contrast, when RPMI8266 were treated with Imatinib of the concentration of 12.8 mol/L, cells grew normally.In comparison to Imatinib, TEB-415, a derivative of Imatinib, can kill H929 MM cells much effectively, its effecacy is only inferior to Bortezomib. RPMI8226, an MM cell line is insensitive to Imatinib, but still sensitive to TEB-415 and its growth can be inhibited by TEB-415.

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