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BI 6727

Cat. No. M1678
BI 6727 Structure
Synonym:

Volasertib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM/1mL In DMSO USD 140 In stock
10mg USD 140 In stock
50mg USD 450 In stock
100mg USD 760 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Customer Product Validations & Biological Datas
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
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
Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 618.81
Formula C34H50N8O3
CAS Number 755038-65-4
Purity >98%
Solubility DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BI 6727, Volasertib supplier, PLK, inhibitors

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