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 19 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 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkn5O|IhcA>? M3O5OGlEPTB;MUewxtE2OSCwTR?= NV3rPINtOjV3N{[wO|Q>
KG-1 NFzIW29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX63NkBp M{nkPGlEPTB;MUWwxtE3PyCwTR?= NYHwdIdHOjV3N{[wO|Q>
MOLM-13 M1XY[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXm3NkBp NXHBTmlPUUN3ME21O:KyPDRibl2= NEHFfo8zPTV5NkC3OC=>
MV-4-11 NY\ZdmRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3hO|IhcA>? NEXUZWJKSzVyPUG2xtE3KG6P NUO1WmRwOjV3N{[wO|Q>
NOMO-1 M2HKbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzaTXc4OiCq MoD0TWM2OD1zNEZCtVchdk1? NHX6WVQzPTV5NkC3OC=>
OCI-AML3 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXUO|IhcA>? M37BSWlEPTB;OUFCtVUyKG6P MX6yOVU4PjB5NB?=
SKM-1 M{jN[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWO3NkBp MkHiTWM2OD17NdMxOVIhdk1? NHv4PIszPTV5NkC3OC=>
THP-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vTW|czKGh? M1\ZUWlEPTB;NUdCtVM6KG6P MYKyOVU4PjB5NB?=
MCF7/LTED  MljuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrrSHAzNjVvNECgcm0> MVe1JIQ> Mny2bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHy2cnUzPTR6MEm0Ny=>
HCC1428/LTED Mli1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TvPVIvPS12MDDuUS=> M3m1N|Uh\A>? M133[IlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYKyOVQ5ODl2Mx?=
A431 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3iR5MyOC1|MDDuUS=> MYqxMVQh\A>? M3rIbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MWCyN|g6OTB7Nh?=
FaDu  MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHhNE0yODByIH7N M370XVEuPCCm MmHybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ NGXHeYszOzh7MUC5Oi=>
SF188 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fxV|UxNTF3MDDuUS=> M37tPVczKGh? NF;t[oVFVVOR NFLySVBqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> M1LmNVI{QDh5NkS1
T98G MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HMPVUxNTF3MDDuUS=> MU[3NkBp MYnEUXNQ MmO4bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NIXHcXczOzh6N{[0OS=>
DU145 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTjNVAwPTBxMkWwJI5O NGPBc3MzPCCq NVywfm1VUUN3MEyxNEBvVQ>? NVHiUGZ6OjN6OES0Nlg>
LNCaP M4XO[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;rblExNzVyL{K1NEBvVQ>? NWPPOmNnOjRiaB?= MmLOTWM2ODxzMDDuUS=> NIG4Um4zOzh6NESyPC=>
PC3 Mn7YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\nXpoyOC93MD:yOVAhdk1? NInMNJIzPCCq NEPa[VRKSzVy4pk8OlAxKG6P NXi5d2p3OjN6OES0Nlg>
RT4 NF;pPJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LGOFQ5KGh? MoLMTWM2OD1zMUGuNlchdk1? MXmyN|c6OjZ|OR?=
5637 Mmj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jVSVQ5KGh? MlL0TWM2OD1zMU[1MlE1KG6P NFnPNGwzOzd7Mk[zPS=>
T24 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XoR|Q5KGh? NEfLOJRKSzVyPUKwOE46OSCwTR?= NFzrSFczOzd7Mk[zPS=>
KMCH-1 MkLWRZBweHSxc3nzJGF{e2G7 NG[wSWwzODBibl2= NILmOXAzPCCq MYrpcoR2[2W|IHHwc5B1d3Orcx?= MorWNlM4ODN4N{O=
Mz-ChA-1 NYHBeJE{SXCxcITvd4l{KEG|c3H5 NGO3XoczODBibl2= M2\1XVI1KGh? MXHpcoR2[2W|IHHwc5B1d3Orcx?= NFLCcJczOzdyM{[3Ny=>
HUCCT-1 M2LZO2Fxd3C2b4Ppd{BCe3OjeR?= MkD0NlAxKG6P NFHWR2UzPCCq M1e4b4lv\HWlZYOgZZBweHSxc3nz MYmyN|cxOzZ5Mx?=
HCT 116 NYjxfpNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;FR|UxyqB;IEKzJI5O MoT4NVk{QDN6MkO=
NCI-H460 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLWbpk3TUN3MNMgQUAzOSCwTR?= NXH4enE6OTl|OEO4NlM>
BRO NVvPcldbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULRZYhbTUN3MNMgQUAyOSCwTR?= NH;tXXYyQTN6M{iyNy=>
GRANTA-519 NEfYTZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTFR|UxyqB;IEG1JI5O M2Trb|E6Ozh|OEKz
HL-60 MlTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU[2b2lpTUN3MNMgQUA{OiCwTR?= M1vuR|E6Ozh|OEKz
THP-1 MnLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DRO2VEPTBiPTCzOkBvVQ>? M2n5V|E6Ozh|OEKz
Raji MmW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHtfphuTUN3MDC9JFM4KG6P NITaUlkyQTN6M{iyNy=>

... 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]
+ 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 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02757248 Withdrawn PTCL|CTCL Anne Beaven MD|National Comprehensive Cancer Network|Boehringer Ingelheim|Duke University November 2016 Phase 1
NCT02722135 Withdrawn Leukemia Myeloid Acute Boehringer Ingelheim November 2016 Phase 1
NCT02527174 Withdrawn 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
NCT02722135 Withdrawn Leukemia Myeloid Acute Boehringer Ingelheim November 2016 Phase 1
NCT02527174 Withdrawn Leukemia Myeloid Acute|Leukemia Monocytic Acute|Leukemia Myelomonocytic Acute|Leukemia Erythroblastic Acute|Leukemia Megakaryoblastic Acute University of Alberta November 2016 Phase 1

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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

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    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

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

  • Rigosertib (ON-01910)

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  • HMN-214

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  • MLN0905

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

  • Ro3280

    RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.

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  • NMS-P937 (NMS1286937)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID