Volasertib (BI 6727)
Molecular Weight(MW): 618.81
Volasertib (BI 6727) is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Phase 3.
Cited by 12 Publications
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Western blot analysis. HeLa or MCF7 cells were treated with nocodazole (noc, 50 ng/ml), paclitaxel (pacli, 50 nM), the Plk1 inhibitor BI 2536 (50 nM) or BI 6727 (50 nM) for 16 h and cellular extracts were prepared for western blot analysis with antibodies as indicated. con: cellular extracts from control cells without any treatment. β-actin served as loading control.
Oncogene 2013 10.1038/onc.2013.518. Volasertib (BI 6727) purchased from Selleck.
Decrease viability of Hec50 subclones after 3 days treatment with BI6727 was shown. Reduction of Cdc2 Tyr15 phosphorylation and increase Histone H3 Ser10 phosphorylation in cells treated with BI 6727 was observed.
Dr. Xiangbing Meng from University of Iowa. Volasertib (BI 6727) purchased from Selleck.
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|Description||Volasertib (BI 6727) is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Phase 3.|
|Features||A high volume of distribution, indicating good tissue penetration, and a long terminal half-life.|
Like BI2536, BI6727 is an ATP-competitive kinase inhibitor from the dihydropteridinone class of compounds. In addition to Plk1, BI6727 also potently inhibits two closely related kinases Plk2 and Plk3 with IC50 of 5 nM and 56 nM, respectively. BI6727 at concentrations up to 10 μM displays no inhibitory activity against a panel of >50 other kinases. BI6727 inhibits the proliferation of multiple cell lines derived from various cancer tissues, including HCT116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1, and Raji cells with EC50 of 23 nM, 21 nM, 11 nM, 15 nM, 32 nM, 36 nM, and 37 nM, respectively. BI6727 treatment (100 nM) in NCI-H460 cells induces an accumulation of mitotic cells with monopolar spindles and positive staining for histone H3 phosphoserine 10, confirming that cells are arrested early in the M phase, followed by induction of apoptosis.  Low nanomolar concentrations of BI6727 display potent inhibitory activity against neuroblastoma (NB) tumor-initiating cells (NB TIC) with EC50 of 21 nM, whereas only micromolar concentrations of BI6727 are cytotoxic for normal pediatric neural stem cells.  BI6727 induces growth arrest of Daoy and ONS-76 medulloblastoma cells similar to BI 2536. 
|In vivo||Administration of BI6727 significantly inhibits the growth of multiple human carcinoma xenografts including HCT116, NCI-H460, and taxane-resistant CXB1 colon carcinoma, accompanied by an increase in the mitotic index as well as an increase in apoptosis.  In in vivo studies, BI6727 shows better toxicity and pharmacokinetic profile compared to BI2536. |
In vitro kinase assays:Recombinant human Plk1 (residues 1-603) is expressed as NH2-terminal, GST-tagged fusion protein using a baculoviral expression system and purified by affinity chromatography using glutathione-agarose. Enzyme activity assays for Plk1 are done in the presence of serially diluted BI6727 using 20 ng of recombinant kinase and 10 μg casein from bovine milk as substrate. Kinase reactions are done in a final volume of 60 μL for 45 minutes at 30 °C [15 mM MgCl2, 25 mM MOPS (pH 7.0), 1 mM DTT, 1% DMSO, 7.5 μM ATP, 0.3 μCi γ-32P-ATP]. Reactions are terminated by the addition of 125 μL of ice-cold 5% TCA. After transferring the precipitates to MultiScreen mixed ester cellulose filter plates, plates are washed with 1% TCA and quantified radiometrically. Dose-response curves are used for calculating IC50 value.
|In vitro||DMSO||20 mg/mL warmed (32.32 mM)|
|In vivo||4% DMSO+corn oil||2mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02722135||Withdrawn||Leukemia, Myeloid, Acute||Boehringer Ingelheim||November 2016||Phase 1|
|NCT02527174||Not yet recruiting||Leukemia, Myeloid, Acute|Leukemia, Monocytic, Acute|Leukemia, Myelomonocytic, Acute|Leukemia, Erythroblastic, Acute|Leukemia, Megakaryoblastic, Acute||University of Alberta||November 2016||Phase 1|
|NCT02757248||Withdrawn||PTCL|CTCL||Anne Beaven, MD|National Comprehensive Cancer Network|Boehringer Ingelheim|Duke University||November 2016||Phase 1|
|NCT02875002||Not yet recruiting||Relapsed and Refractory Aggressive B- and T-cell Lymphomas|Lymphoma||Yale University|Massey Cancer Center|Sidney Kimmel Comprehensive Cancer Center||October 2016||Phase 1|
|NCT02905994||Not yet recruiting||AML||Massachusetts General Hospital|Boehringer Ingelheim||September 2016||Phase 1|
|NCT02861040||Withdrawn||Recurrent Adult Acute Lymphoblastic Leukemia|Refractory Adult Acute Lymphoblastic Leukemia||Northwestern University|National Comprehensive Cancer Network|National Cancer Institute (NCI)||August 2016||Phase 1|
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