使用浓度 【具体使用浓度请参考相关文献,并根据自身实验条件(如实验目的,细胞种类,培养特性等)进行摸索和优化。】 相关实验(数据来自于公开发表的文献,仅供参考) (一)细胞实验(体外研究) 为检测BI 6727在细胞中的作用,用100 nM BI 6727处理NCI-H460细胞24 h,发现有丝分裂细胞聚集,细胞中有单极纺锤体和组蛋白H3的磷酸丝氨酸10阳性染色,表明细胞处于M期,随后诱导细胞凋亡。[1] (二)动物实验(体内研究) 在体内实验中,给HCT116移植瘤小鼠静脉注射BI 6727(15、20、25 mg/kg),BI 6727引起显著的肿瘤延迟,甚至肿瘤衰退。[1] 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).
[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).