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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Cited by 46 Publications

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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 NXnPRml3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTjRnk4PzJiaB?= NF\uTWRKSzVyPUG3NOKyPTFibl2= M1LX[FI2PTd4MEe0
KG-1 MmToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjvXZE4OiCq M3;Rc2lEPTB;MUWwxtE3PyCwTR?= M3XtUFI2PTd4MEe0
MOLM-13 M1[1eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfwWXc4OiCq MlvZTWM2OD13N9MxOFQhdk1? M2nxVlI2PTd4MEe0
MV-4-11 Mn7kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PRVVczKGh? NH3JfolKSzVyPUG2xtE3KG6P MlvCNlU2PzZyN{S=
NOMO-1 MlPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnsVXo4OiCq MVrJR|UxRTF2NdMxO{BvVQ>? MWGyOVU4PjB5NB?=
OCI-AML3 NUnsVFRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWW3NkBp NILmd2dKSzVyPUmwxtE2OSCwTR?= MkTpNlU2PzZyN{S=
SKM-1 M2P5[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLzO|IhcA>? MnzkTWM2OD17NdMxOVIhdk1? NF64NYUzPTV5NkC3OC=>
THP-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWS3NkBp M2\BVmlEPTB;NUdCtVM6KG6P MmDxNlU2PzZyN{S=
MCF7/LTED  M4XVdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;6UmhmOi53LUSwJI5O NYr1dWxGPSCm NVLqVJNGcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlH0NlU1QDB7NEO=
HCC1428/LTED NFn0ZYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmT4Nk42NTRyIH7N M{PySVUh\A>? MleybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHLGb3MzPTR6MEm0Ny=>
A431 M1vUPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnn3NE0{OCCwTR?= M1r5TVEuPCCm NUfqRVV1cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCCmb4PlMUBidmRidHnt[U1l\XCnbnTlcpQhdWGwbnXy MY[yN|g6OTB7Nh?=
FaDu  MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjHOXIxNTFyMECgcm0> M3K4e|EuPCCm MX;pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? NI[wSI8zOzh7MUC5Oi=>
SF188 Mn36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHlOVAuOTVyIH7N M1GxSFczKGh? NEGwUXZFVVOR NUL1NHVqcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NIDlNYQzOzh6N{[0OS=>
T98G NW\EVVN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;sOFUxNTF3MDDuUS=> M{PjN|czKGh? Mmf6SG1UVw>? Mn\vbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MVGyN|g5PzZ2NR?=
DU145 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPpPGkyOC93MD:yOVAhdk1? M4H4WFI1KGh? NVTjfGFjUUN3MEyxNEBvVQ>? MYiyN|g5PDR{OB?=
LNCaP NXvOb2l3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUexNE82OC9{NUCgcm0> NXvqUXR4OjRiaB?= M{HWWGlEPTB:MUCgcm0> M1vaVVI{QDh2NEK4
PC3 M2\Udmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmT3NVAwPTBxMkWwJI5O MoTwNlQhcA>? MUnJR|Ux6oj:NkCwJI5O M3rmclI{QDh2NEK4
RT4 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{D1NFQ5KGh? NVTkeG9{UUN3ME2xNVEvOjdibl2= M3\nRVI{Pzl{NkO5
5637 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfpOHk1QCCq NEXDd3dKSzVyPUGxOlUvOTRibl2= M3vZ[|I{Pzl{NkO5
T24 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\6S3c1QCCq M1jPbmlEPTB;MkC0MlkyKG6P NX\pSo13OjN5OUK2N|k>
KMCH-1 MULBdI9xfG:|aYOgRZN{[Xl? MnvMNlAxKG6P MV6yOEBp MnvSbY5lfWOnczDhdI9xfG:|aYO= MoW4NlM4ODN4N{O=
Mz-ChA-1 NWTlPFVLSXCxcITvd4l{KEG|c3H5 NXi4TWdsOjByIH7N NVrweYF6OjRiaB?= M3rYOYlv\HWlZYOgZZBweHSxc3nz M2jBWlI{PzB|Nkez
HUCCT-1 MXvBdI9xfG:|aYOgRZN{[Xl? NULGcXQxOjByIH7N MkDaNlQhcA>? M3f3eIlv\HWlZYOgZZBweHSxc3nz NF7ZdZIzOzdyM{[3Ny=>
HCT 116 NELOfIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnFR|UxyqB;IEKzJI5O NUXHe4R7OTl|OEO4NlM>
NCI-H460 NIq4VFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjFR|UxyqB;IEKxJI5O NGfWe4UyQTN6M{iyNy=>
BRO Ml3jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPLSWM2OMLiPTCxNUBvVQ>? NFjl[msyQTN6M{iyNy=>
GRANTA-519 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjFR|UxyqB;IEG1JI5O M1PPRlE6Ozh|OEKz
HL-60 MnfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrFR|UxyqB;IEOyJI5O NHjYNXAyQTN6M{iyNy=>
THP-1 NVLtOWhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjZfItYTUN3MDC9JFM3KG6P M4TkOlE6Ozh|OEKz
Raji MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDJe3psTUN3MDC9JFM4KG6P M{D2UFE6Ozh|OEKz

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-PLK1 / PLK1; 

PubMed: 29108241     


The protein expression of PLK1 and its phosphorylation levels at 24 hours after volasertib treatment in HL-60 and K562 cells.

p-AKT / AKT / p-MAPK / MAPK; 

PubMed: 29108241     


Phosphorylation levels of AKT and MAPK in AML cell lines after volasertib administration.

PARP / c-myc; 

PubMed: 29383095     


Treatment with volasertib (24 hours) induces PARP cleavage and decreases total c-myc expression in the indicated lymphoma cell lines. From left to right: diffuse large B-cell lymphomas (DLBCL), anaplastic large cell lymphoma (ALCL), cutaneous T-cell lymphoma (CTCL) and, peripheral T-cell lymphomas non-otherwise specified (PTCL-NOS). Protein expression was evaluated by immunoblotting.

p-c-Met / c-Met / p-FAK / FAK / p-Src / Src ; 

PubMed: 31040125     


The same cell lines treated identically were subjected to immunoblotting for the indicated proteins (upper) with densitometric quantification normalized with b-actin (lower).

Fibronectin / β-integrin / p-vimentin / Vimentin / p-HH3; 

PubMed: 31040125     


Epithelial and mesenchymal non-small-cell lung cancer (NSCLC) cell lines after treatment with 50 nM volasertib for 24 h. Cells were then harvested, and lysates were immunoblotted for the indicated proteins.

29108241 29383095 31040125
Immunofluorescence
PLK1 / Wee1; 

PubMed: 29108241     


The protein expressions of PLK1 and Wee1 were evaluated by immunofluorescent staining. Both parental and volasertib-resistant MOLM14 and HL-60 cells were treated with 50 nM volasertib for 18 hours.

29108241
Growth inhibition assay
Cell viability; 

PubMed: 29383095     


Survival of different B-cell and T-cell lymphoma cell lines upon treatment with indicated doses of Volasertib at 72 hrs. 

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

Kinase Assay:[1]
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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]
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  • 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]
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  • 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 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 powder
in solvent
Synonyms N/A

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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

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.

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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.

selleck catalog

PLK Signaling Pathway Map

PLK Inhibitors with Unique Features

  • Pan Plk Inhibitors

    BI 2536 : Pan-Plk1, Plk1, IC50=0.83 nM; Plk2, IC50=3.5 nM; Plk3, IC50=9 nM.

  • Most Potent Plk Inhibitor

    BI 2536 : Plk1, IC50=0.83 nM.

  • Plk Inhibitor in Clinical Trial

    Rigosertib (ON-01910) : Phase III for Myelo Dysplastic Syndrome (MDS).

  • Newest Plk Inhibitor

    Ro3280 New : Potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.

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  • BI 2536

    BI2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. It shows 4- and 11-fold greater selectivity against Plk2 and Plk3. Phase 2.

    Features:The first potent and selective Plk1 inhibitor that induces all hallmarks of Plk1 inhibition.

  • Rigosertib (ON-01910)

    Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Phase 3.

  • HMN-214

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  • MLN0905

    MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.

  • Ro3280

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID