BI 2536是一种新型、强效的、高选择性PLK1抑制剂(IC50=0.83 nM),也可以抑制PLK2 (IC50=3.5 nM)和PLK3 (IC50= 9.0 nM)。BI 2536诱导细胞有丝分裂阻断,并诱导癌细胞凋亡,另外,还可以抑制裸鼠体内移植瘤生长,诱导肿瘤衰退。BI 2536作用于AML细胞表现出强效的抗增殖作用。
目前,BI 2536已用于临床Phase I/II研究。
【该产品仅用于科研实验,不能用于人体】
参考文献
[1] Steegmaier M, et al. BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo. Curr Biol, 17(4): 316-322 (2007).
[2] Lu B, et al. The Plk1 Inhibitor BI 2536 Temporarily Arrests Primary Cardiac Fibroblasts in Mitosis and Generates Aneuploidy In Vitro. PLoS ONE 5(9): e12963 (2010).
[3] Patrick Schöffski, et al. Polo-Like Kinase (PLK) Inhibitors in Preclinical and Early Clinical Development in Oncology. The Oncologist 14(6): 559-570 (2009).
[4] Lee KH, et al. Polo-Like Kinase-1 (Plk-1) Inhibitor BI 2536 Induces Mitotic Arrest and Apoptosis in Vivo: First Demonstration of Target Inhibition in the Bone Marrow of AML Patients. Blood 112: 2641 (2008).
冰袋运输。粉末直接保存于-20 ºC,有效期2年。溶于DMSO、乙醇。建议分装后-20ºC避光保存,避免反复冻存,至少可存放6个月。