Volasertib (BI 6727)

Catalog No.S2235

For research use only.

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. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3.

Volasertib (BI 6727) Chemical Structure

CAS No. 755038-65-4

Selleck's Volasertib (BI 6727) has been cited by 128 publications

Purity & Quality Control

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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. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. 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 MojFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3NNVA4OiCq M{HMW2lEPTB;MUewxtE2OSCwTR?= NVu2[4c6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1O|YxPzRpPkK1OVc3ODd2PD;hQi=>
KG-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXW3NkBp M1e4emlEPTB;MUWwxtE3PyCwTR?= M3XGPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUe2NFc1Lz5{NUW3OlA4PDxxYU6=
MOLM-13 NVfuTY4{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjvO|IhcA>? NIXMfolKSzVyPUW3xtE1PCCwTR?= NF7vWXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW3OlA4PCd-MkW1O|YxPzR:L3G+
MV-4-11 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;HWpA4OiCq NWS2XXU{UUN3ME2xOuKyPiCwTR?= M2TOdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUe2NFc1Lz5{NUW3OlA4PDxxYU6=
NOMO-1 NYTuVo5ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrEO|IhcA>? NWqxTGtpUUN3ME2xOFXDuTdibl2= NU\TdnF6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1O|YxPzRpPkK1OVc3ODd2PD;hQi=>
OCI-AML3 M3zOcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGX2RXo4OiCq NYPkWJVzUUN3ME25NOKyPTFibl2= M2iwS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUe2NFc1Lz5{NUW3OlA4PDxxYU6=
SKM-1 MmG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3QXoxnPzJiaB?= Mom1TWM2OD17NdMxOVIhdk1? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV5NkC3OEc,OjV3N{[wO|Q9N2F-
THP-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mon1O|IhcA>? MVXJR|UxRTV4wsGzPUBvVQ>? M2DEZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUe2NFc1Lz5{NUW3OlA4PDxxYU6=
MCF7/LTED  Ml\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVmyMlUuPDBibl2= MVG1JIQ> MVrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR6MEm0N{c,OjV2OEC5OFM9N2F-
HCC1428/LTED MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXpRotlOi53LUSwJI5O MmrCOUBl NVrYRoc4cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHXKOG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS4NFk1Oyd-MkW0PFA6PDN:L3G+
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LNCaP NGnUWlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoG2NVAwPTBxMkWwJI5O NGXicnozPCCq NHnnc|NKSzVyPEGwJI5O NVvydllkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4PFQ1OjhpPkKzPFg1PDJ6PD;hQi=>
PC3 M{TMc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUmxNE82OC9{NUCgcm0> NF:3OIYzPCCq MoXNTWM2OOLKvE[wNEBvVQ>? M{HaOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEi0OFI5Lz5{M{i4OFQzQDxxYU6=
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HUCCT-1 NIf4dm5CeG:ydH;zbZMhSXO|YYm= M3n4cFIxOCCwTR?= NXfmNYxGOjRiaB?= NELrWGxqdmS3Y3XzJIFxd3C2b4Ppdy=> NIWxdpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{ewN|Y4Oyd-MkO3NFM3PzN:L3G+
HCT 116 NUPw[pU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PUVGVEPTEEoE2gNlMhdk1? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTN6M{iyN{c,OTl|OEO4NlM9N2F-
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HL-60 NI\0PGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXOzeFRqTUN3MNMgQUA{OiCwTR?= MojqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl|OEO4NlMoRjF7M{izPFI{RC:jPh?=
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Rh30 NY\LTJMzeUiWUzDhd5NigQ>? NUHacXNGeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoN|Ah[2WubIO= M4fITFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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NB-EBc1 MYrxTHRUKGG|c3H5 M2fYSJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz NWX3Z4pmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 NWLCbZFOeUiWUzDhd5NigQ>? MmS4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 NXPQS|UyeUiWUzDhd5NigQ>? MVPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SKBR3 MXTDfZRwfG:6aXPpeJkh[XO|YYm= MXSyOEBpenN? MnvKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfS=> NYnSV2s5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDhpPkK5Nlg5QTR6PD;hQi=>
MDA-MB-231 NWLnTJBMS3m2b4TvfIlkcXS7IHHzd4F6 MnHZNlQhcHK| NILvdmJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYm= NFHFfXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1QCd-MkmyPFg6PDh:L3G+
MDA-MB-468 MYjDfZRwfG:6aXPpeJkh[XO|YYm= MkHHNlQhcHK| NXrlN4t5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ3QCClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5 NWPvVpFMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDhpPkK5Nlg5QTR6PD;hQi=>
BT474 MUTDfZRwfG:6aXPpeJkh[XO|YYm= M1vlVVI1KGi{cx?= NXL4eJZHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSlR2N{SgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigQ>? Ml:4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFgoRjJ7Mki4PVQ5RC:jPh?=
ZR-75-1 M2rqb2N6fG:2b4jpZ4l1gSCjc4PhfS=> MmDxNlQhcHK| NX;5eZlnS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hYlJvN{WtNUBk\WyuczDh[pRmeiB{NDDodpMh[nliTWTUJIF{e2G7 M4nXclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQ5Lz5{OUK4PFk1QDxxYU6=
Assay
Methods Test Index PMID
Western blot p-PLK1 / PLK1 ; p-AKT / AKT / p-MAPK / MAPK ; PARP / c-myc ; p-c-Met / c-Met / p-FAK / FAK / p-Src / Src ; Fibronectin / β-integrin / p-vimentin / Vimentin / p-HH3 29108241 29383095 31040125
Immunofluorescence PLK1 / Wee1 29108241
Growth inhibition assay Cell viability 29383095
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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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]
  • Animal Models: Female BomTac:NMRI-Foxn1nu mice grafted s.c. with HCT116, NCI-H460, or CXB1 cells
  • 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 to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+corn oil
For best results, use promptly after mixing.

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 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1C(=O)N(C2=CN=C(N=C2N1C(C)C)NC3=C(C=C(C=C3)C(=O)NC4CCC(CC4)N5CCN(CC5)CC6CC6)OC)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02722135 Withdrawn Drug: Volasertib Leukemia Myeloid Acute Boehringer Ingelheim November 2016 Phase 1
NCT02721875 Terminated Drug: Volasertib|Drug: Azacitidine Myelodysplastic Syndromes Boehringer Ingelheim April 28 2016 Phase 1
NCT02201329 Completed Drug: Azacitidine|Drug: Volasertib Myelodysplastic Syndromes|Leukemia Myelomonocytic Chronic Boehringer Ingelheim August 2014 Phase 1
NCT01971476 Completed Drug: volasertib Leukemia|Neoplasms Boehringer Ingelheim October 22 2013 Phase 1
NCT01662505 Completed Drug: Volasertib Leukemia Myeloid Acute Boehringer Ingelheim August 2012 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

Tel: +1-832-582-8158 Ext:3
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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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