Saracatinib (AZD0530) is a potent modulator of ABCB1-mediated multidrug resistance in vitro and in vivo
Saracatinib,a highly selective,dual Sre/Abl kinase inhibitor,is currently in a Phase Ⅱ clinical trial for the treatment of ovarian cancer.In our study,we investigated the effect of saracatinib on the reversal of multidrug resistance (MDR) induced by ATP-binding cassette (ABC) transporters in vitro and in vivo.Our results showed that saracatinib significantly enhanced the cytotoxicity of ABCB1 substrate drugs in ABCB1 overexpressing HeLa/v200,MCF-7/adr and HEK293/ABCB1 cells,an effect that was stronger than that ofgefitinib,whereas it had no effect on the cytotoxicity of the substrates in ABCC1 overexpressing HL-60/adr cells and its parental sensitive cells.
Ke-jun Liu Hai-Ying Wu
State Key Laboratory of Oncology in Southern China,Cancer Center,Sun Yat-Sen University,Guangzhou 510060,People”s Republic of China
国内会议
2012医学科学前沿暨第二届个体化治疗与抗肿瘤药物研究新趋向研讨会
深圳
英文
450-450
2012-07-13（万方平台首次上网日期，不代表论文的发表时间）