Volasertib (BI 6727)

Catalog No.S2235

Volasertib (BI 6727) Chemical Structure

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.

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In DMSO USD 202 In stock
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5 Customer Reviews

  • 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.

    immunoblot analyses were performed in A375 xenografted melanoma tissues treated with BI 6727 (10 and 25 mg/kg body weight) or vehicle alone to determine the effect of PLK1 knockdown using (D) PCK1 and (E) FBP1 antibodies. The blots were re-probed with b-actin for loading control. Data is representative of three individual experiments. (For interpretation of the references to colour in this figure legend, the reader is referred to the web version of this article)

    Cancer Lett, 2017, 394:13-21. Volasertib (BI 6727) purchased from Selleck.

  • HNSCC cell-cycle stages determined according to 7-aminoactinomycin D and BrdU incorporation.

    Cancer Lett, 2017, 392:71-82. 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.

  • Hec50 cells are arrested in mitosis after 24hours treatment with 10nM BI 6727.

    Dr. Xiangbing Meng from University of Iowa. Volasertib (BI 6727) purchased from Selleck.

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Biological Activity

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.
Targets
PLK1 [1]
(Cell-free assay)
0.87 nM
In vitro

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. [1] 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. [2] BI6727 induces growth arrest of Daoy and ONS-76 medulloblastoma cells similar to BI 2536. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KASUMI-1 M1zYd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLURpk4OiCq NV\BXZg{UUN3ME2xO|DDuTVzIH7N NFPQeGozPTV5NkC3OC=>
KG-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPj[no4OiCq Ml3BTWM2OD1zNUFCtVY4KG6P NYfjO5Q5OjV3N{[wO|Q>
MOLM-13 NV3vbY95T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYn5Nno3PzJiaB?= M2rhWmlEPTB;NUhCtVQ1KG6P MWCyOVU4PjB5NB?=
MV-4-11 MmfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDiUIg1PzJiaB?= NX;mVIh[UUN3ME2xOuKyPiCwTR?= MUmyOVU4PjB5NB?=
NOMO-1 NUfY[mhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXyxb3dxPzJiaB?= Mn76TWM2OD1zNEZCtVchdk1? M{nBeVI2PTd4MEe0
OCI-AML3 M4e0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoCwO|IhcA>? MX3JR|UxRTlywsG1NUBvVQ>? NYj0XZZFOjV3N{[wO|Q>
SKM-1 MlywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTme|A4OiCq M4HpdWlEPTB;OUZCtVUzKG6P NIrCVHkzPTV5NkC3OC=>
THP-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHNO|IhcA>? M13wNmlEPTB;NUdCtVM6KG6P NF3tc|AzPTV5NkC3OC=>
MCF7/LTED  M17UVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXaNk42NTRyIH7N MV[1JIQ> NWHwfmd3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MUiyOVQ5ODl2Mx?=
HCC1428/LTED M1W4SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljpNk42NTRyIH7N MUC1JIQ> M2Xlb4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1HaXlI2PDhyOUSz
A431 M4jhUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXjepNGOC1|MDDuUS=> Moj2NU01KGR? NUX4fFhQcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCCmb4PlMUBidmRidHnt[U1l\XCnbnTlcpQhdWGwbnXy NX7MdXhJOjN6OUGwPVY>
FaDu  M{HxTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmwMVExODBibl2= MkPMNU01KGR? NIHaT4ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NWjFV4RpOjN6OUGwPVY>
SF188 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2CySFUxNTF3MDDuUS=> NHvacm84OiCq M1TkNGROW09? NFLDN|ZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NWDmV3RwOjN6OEe2OFU>
T98G NFS4OoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYi1NE0yPTBibl2= M13wZlczKGh? MYDEUXNQ MWXpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= M2CwZVI{QDh5NkS1
DU145 Mof0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1u4RVExNzVyL{K1NEBvVQ>? NXLpWmdCOjRiaB?= NELaTVRKSzVyPEGwJI5O M1HwPVI{QDh2NEK4
LNCaP M3naNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\Z[W0yOC93MD:yOVAhdk1? NVe2S2JEOjRiaB?= MX;JR|UxRDFyIH7N NXHhTnBYOjN6OES0Nlg>
PC3 MnuxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{H6fFExNzVyL{K1NEBvVQ>? MnvmNlQhcA>? MkDPTWM2OOLKvE[wNEBvVQ>? MkDnNlM5QDR2Mki=
RT4 NW\pRm5tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFuzeJA1QCCq M13KVGlEPTB;MUGxMlI4KG6P MWiyN|c6OjZ|OR?=
5637 NYG4VWtwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPTPHRPPDhiaB?= MmDXTWM2OD1zMU[1MlE1KG6P NIrkRWYzOzd7Mk[zPS=>
T24 MlfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWK0PEBp M3\0cWlEPTB;MkC0MlkyKG6P NYn4OnczOjN5OUK2N|k>
KMCH-1 MnraRZBweHSxc3nzJGF{e2G7 M{Pxb|IxOCCwTR?= M4LYb|I1KGh? MnXvbY5lfWOnczDhdI9xfG:|aYO= NYjKVYk5OjN5MEO2O|M>
Mz-ChA-1 M3;ocGFxd3C2b4Ppd{BCe3OjeR?= NYDWT4kxOjByIH7N NWP5RXl[OjRiaB?= MVLpcoR2[2W|IHHwc5B1d3Orcx?= NFuzZ|YzOzdyM{[3Ny=>
HUCCT-1 NXPMS3Q4SXCxcITvd4l{KEG|c3H5 MWmyNFAhdk1? MnzhNlQhcA>? NYrWeYNTcW6mdXPld{BieG:ydH;zbZM> NH;6VGszOzdyM{[3Ny=>
HCT 116 NHGxSodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3r3OmVEPTEEoE2gNlMhdk1? MYWxPVM5Ozh{Mx?=
NCI-H460 MoPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXFR|UxyqB;IEKxJI5O M2rsdVE6Ozh|OEKz
BRO NIDYNYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLvSWM2OMLiPTCxNUBvVQ>? NF7ibZQyQTN6M{iyNy=>
GRANTA-519 MmTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTHPWpKTUN3MNMgQUAyPSCwTR?= M3vzelE6Ozh|OEKz
HL-60 Mn24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfuSWM2OMLiPTCzNkBvVQ>? MmDTNVk{QDN6MkO=
THP-1 NX7ifJdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjoVoZKTUN3MDC9JFM3KG6P MmDUNVk{QDN6MkO=
Raji NGXhWoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XPcGVEPTBiPTCzO{BvVQ>? MU[xPVM5Ozh{Mx?=

... Click to View More Cell Line Experimental Data

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. [1] In in vivo studies, BI6727 shows better toxicity and pharmacokinetic profile compared to BI2536. [3]

Protocol

Kinase Assay:[1]
+ Expand

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.
Cell Research:[1]
+ Expand
  • Cell lines: HCT116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1, and Raji
  • Concentrations: Dissolved in DMSO, final concentrations ~1 μM
  • Incubation Time: 24, 48, and 72 hours
  • Method: Cell proliferation assays are done by incubating cells in the presence of various concentrations of BI6727 for 24, 48, and 72 hours and cell growth is assessed by measuring Alamar blue dye conversion in a fluorescence spectrophotometer. Effective concentrations at which cellular growth is inhibited by 50% (EC50) are extrapolated from the dose-response curve fit. To determine the DNA content, cell suspensions are fixed in 80% ethanol, treated for 5 minutes with 0.25% Triton X-100 in PBS, and incubated with 0.1% RNase and 10 μg/mL propidium iodide in PBS for 20 minutes at room temperature. Cell cycle profiles are determined by flow cytometric analysis.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Female BomTac:NMRI-Foxn1nu mice grafted s.c. with HCT116, NCI-H460, or CXB1 cells
  • Formulation: Formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl, or suspended in 0.5% Natrosol 250 hydroxyethyl-cellulose
  • Dosages: ~25 mg/kg/day
  • Administration: Injected i.v., or given intragastrally via gavage needle
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 20 mg/mL warmed (32.32 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
4% DMSO+corn oil
2mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 618.81
Formula

C34H50N8O3

CAS No. 755038-65-4
Storage powder
Synonyms N/A

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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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    I wonder how to reconstitute the inhibitor for in vivo studies?

  • Answer:

    Volasertib can be dissolved in 4% DMSO+Corn oil at 2mg/ml for i.p. injection in mice. For oral administration, it can be formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl, or suspended in 0.5% Natrosol 250 hydroxyethyl-cellulose as indicated in the publications. We also suggest the vehicle 30% PEG400/0.5% Tween80/5% propylene glycol for a suspension which we tested in house.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID