BI 6727 (Volasertib) is a small highly potent Polo-like kinase inhibitor (Plk) with an IC50 of 0 .87 nM and EC50 of 11-37 nM on a panel of cancer cell lines, which exhibited significant anti-proliferative in multiple cancer models, including a model of taxane-resistant colorectal cancer. BI 6727 (Volasertib) caused programmed cell death in colon and non-small cell lung cancer cells both in vitro and in vivo.
|Cell lines||HCT116 and NCI-H460 cells|
|Preparation method||Cell culture and proliferation assays. Cancer cell lines were obtained from the American Type Culture Collection or the German National Resource Center for Biological Material and were cultured according to the supplier’s instructions. Cell proliferation assays were done by incubating cells in the presence of various concentrations of BI 6727 for 72 h and cell growth was assessed by measuring Alamar blue dye (Serotec) conversion in a fluorescence spectrophotometer. Effective concentrations at which cellular growth was inhibited by 50% (EC50) were extrapolated from the dose-response curve fit.|
|Incubation time||72 h|
|Animal models||nude mice bearing established HCT116 human colon carcinoma tumors xenograft model|
|Formulation||formulated in hydrochloric acid (0.1 N), diluted with 0.9% NaCl|
|Administration||i.v. into the tail vein|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
A phase I, dose-escalation study of the novel Polo-like kinase inhibitor volasertib (BI 6727) in patients with advanced solid tumours.
Schöffski et al. Eur J Cancer. 2012 Jan;48(2):179-86. PMID: 22119200.
Small molecule kinase inhibitor screen identifies polo-like kinase 1 as a target for neuroblastoma tumor-initiating cells.
Grinshtein et al. Cancer Res. 2011 Feb 15;71(4):1385-95. PMID: 21303981.
BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity.
Rudolph et al. Clin Cancer Res. 2009 May 1;15(9):3094-102. PMID: 19383823.
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