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.
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Source | Target Oncol (2015). Figure 1. BI 6727 |
| Method | Western blotting | |
| Cell Lines | TC-71 cells | |
| Concentrations | 15 nM | |
| Incubation Time | 48 hr | |
| Results | We found that BI 6727/VCR-mediated apoptosis was significantly decreased in the presence of zVAD.fmk in four of the five tested ES cell lines, while the tendency of zVAD.fmk to reduce BI 6727/ VCR-induced apoptosis in TC-71 ES cells did not reach statistical significance |
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Source | Target Oncol (2015). Figure 1. BI 6727 |
| Method | Apoptosis assay | |
| Cell Lines | ES cells | |
| Concentrations | 15 nM | |
| Incubation Time | 48 h | |
| Results | Interestingly, suboptimal doses of BI 6727 and VCR synergized to trigger DNA fragmentation, used as a typical parameter to assess apoptosis |
| Cell Experiment | |
|---|---|
| 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. |
| Concentrations | 0~100µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| 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 |
| Dosages | 40 mg/kg |
| Administration | i.v. into the tail vein |
| Molecular Weight | 618.81 |
| Formula | C34H50N8O3 |
| CAS Number | 755038-65-4 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage | 2-8°C, protect from light |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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