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
USD 120 In stock

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3 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.

    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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 M333e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nPfFczKGh? MmHPTWM2OD1zN{FCtVUyKG6P MUmyOVU4PjB5NB?=
KG-1 NHTQVJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW[3NkBp NYj2OFlUUUN3ME2xOVDDuTZ5IH7N NWjuXFRqOjV3N{[wO|Q>
MOLM-13 Mo\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfSO|IhcA>? NU\NPWV4UUN3ME21O:KyPDRibl2= Ml\WNlU2PzZyN{S=
MV-4-11 NGnwbFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTSO|IhcA>? M{jTRmlEPTB;MUdCtVYhdk1? NYjqelNZOjV3N{[wO|Q>
NOMO-1 NYXSdVBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\tdFczKGh? NXrxUY5LUUN3ME2xOFXDuTdibl2= NFnRTZYzPTV5NkC3OC=>
OCI-AML3 M2nqb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVW3NkBp MW\JR|UxRTlywsG1NUBvVQ>? MWOyOVU4PjB5NB?=
SKM-1 NXPD[mlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnUZ4JjPzJiaB?= MYHJR|UxRTl3wsG1NkBvVQ>? MmrWNlU2PzZyN{S=
THP-1 NYjFUmxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXW3NkBp MXHJR|UxRTV4wsGzPUBvVQ>? MYCyOVU4PjB5NB?=
MCF7/LTED  M37ZZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlj1Nk42NTRyIH7N NGq4d4s2KGR? NYXWNVB2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MV6yOVQ5ODl2Mx?=
HCC1428/LTED MlfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17uN|IvPS12MDDuUS=> MUG1JIQ> MoDLbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFT2N3AzPTR6MEm0Ny=>
A431 NXPQS3h7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzJWpkxNTNyIH7N M1n2NVEuPCCm M1rLU4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M13J[lI{QDlzMEm2
FaDu  M3fGfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjWe2xFOC1zMECwJI5O MnXtNU01KGR? MkjGbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ MWGyN|g6OTB7Nh?=
SF188 NI\2OZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU[1NE0yPTBibl2= MnHKO|IhcA>? MlXKSG1UVw>? NVHlclNqcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NUHxb4dROjN6OEe2OFU>
T98G NIjEbnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\sOVAuOTVyIH7N NWj4Vnp6PzJiaB?= NVrQPGhCTE2VTx?= MX\pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MnjKNlM5QDd4NEW=
DU145 M3;EUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXm3b3RpOTBxNUCvNlUxKG6P M3;zZlI1KGh? M2HGUmlEPTB:MUCgcm0> NHXQcGMzOzh6NESyPC=>
LNCaP MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWO5VGpSOTBxNUCvNlUxKG6P M3LpTVI1KGh? M1m1SGlEPTB:MUCgcm0> NXnyV4lsOjN6OES0Nlg>
PC3 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoH5NVAwPTBxMkWwJI5O M1f3cVI1KGh? M2DFXWlEPTEkiMy2NFAhdk1? MlfHNlM5QDR2Mki=
RT4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\sOFghcA>? NFLR[oRKSzVyPUGxNU4zPyCwTR?= NIj4PWczOzd7Mk[zPS=>
5637 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPYcZNHPDhiaB?= NVS1elF2UUN3ME2xNVY2NjF2IH7N M4rm[|I{Pzl{NkO5
T24 NEfm[|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYruZ2VjPDhiaB?= M2PxU2lEPTB;MkC0MlkyKG6P NXfYUmFxOjN5OUK2N|k>
KMCH-1 NYD5dG9GSXCxcITvd4l{KEG|c3H5 MmTPNlAxKG6P M3rpb|I1KGh? NV3xc|lYcW6mdXPld{BieG:ydH;zbZM> M{mxXVI{PzB|Nkez
Mz-ChA-1 Mkj4RZBweHSxc3nzJGF{e2G7 NWLSU3c4OjByIH7N MUKyOEBp MoLXbY5lfWOnczDhdI9xfG:|aYO= NU\XdJdCOjN5MEO2O|M>
HUCCT-1 NHzm[FlCeG:ydH;zbZMhSXO|YYm= Mn;BNlAxKG6P MlzKNlQhcA>? NIjVWFJqdmS3Y3XzJIFxd3C2b4Ppdy=> NFzhSXUzOzdyM{[3Ny=>
HCT 116 MmGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3SzS2VEPTEEoE2gNlMhdk1? M3rz[|E6Ozh|OEKz
NCI-H460 NX;reoFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mni4SWM2OMLiPTCyNUBvVQ>? MlvONVk{QDN6MkO=
BRO NXjVdoFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nIdWVEPTEEoE2gNVEhdk1? M1zWTFE6Ozh|OEKz
GRANTA-519 NWTOfndDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NECwWnNGSzVywrC9JFE2KG6P NWnMcGdbOTl|OEO4NlM>
HL-60 NUnHOZh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;FR|UxyqB;IEOyJI5O NXL0cGxuOTl|OEO4NlM>
THP-1 NWXGN45UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LNb2VEPTBiPTCzOkBvVQ>? MkjGNVk{QDN6MkO=
Raji MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;FfmVEPTBiPTCzO{BvVQ>? Mo\ZNVk{QDN6MkO=

... 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
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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
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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
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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 (32.32 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+corn oil 2mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
NCT02722135 Not yet recruiting Leukemia, Myeloid, Acute Boehringer Ingelheim August 2016 Phase 1
NCT02757248 Not yet recruiting PTCL|CTCL Anne Beaven, MD|National Comprehensive Cancer Network|Boehringer Ingelheim|Duke University July 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 June 2016 Phase 1
NCT02721875 Recruiting Myelodysplastic Syndromes Boehringer Ingelheim April 2016 Phase 1
NCT02198482 Recruiting Acute Myeloid Leukemia (AML)|High-risk Myelodysplastic Syndrome (MDS) University of Ulm February 2016 Phase 2
NCT02201329 Completed Myelodysplastic Syndromes|Leukemia, Myelomonocytic, Chronic Boehringer Ingelheim August 2014 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID