BI6727又称为BI-6727、Volasertib,是一种高度有效的、ATP竞争性PLK1抑制剂,IC50为0.87 nM,比作用于PLK2和PLK3选择性高6和65倍,IC50分别为5 nM和56 nM。BI6727对多种癌细胞具有明显的抗肿瘤活性,抑制多种细胞增殖,包括HCT 116(EC50=23 nM)、NCI-H460(EC50=21 nM)和BRO(EC50=11 nM)等,并抑制体内移植瘤生长。另外,BI6727还可以抑制bromodomain和BRD4蛋白活性。
目前,BI6727已用于临床Phase 3研究阶段。
【该产品仅用于科研实验,不能用于人体】
参考文献
[1] Rudolph D, et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity. Clin Cancer Res. 15(9): 3094-3102 (2009).
[2] Grinshtein N, et al. Small molecule kinase inhibitor screen identifies polo-like kinase 1 as a target for neuroblastoma tumor-initiating cells. Cancer Res. 71(4): 1385-1395 (2011).
[3] Gjertsen BT, et al. Discovery and development of the Polo-like kinase inhibitor volasertib in cancer therapy. Leukemia 29: 11–19 (2015).
[4] Kumar S, et al. PLK-1 Targeted Inhibitors and Their Potential against Tumorigenesis. Biomed Res Int. (2015).
冰袋运输。粉末直接保存于-20 ºC,有效期2年。溶于DMSO。建议分装后-20ºC避光保存,避免反复冻存,至少可存放6个月。