Volasertib (BI 6727)

For research use only.

Catalog No.S2235

89 publications

Volasertib (BI 6727) Chemical Structure

CAS No. 755038-65-4

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) RMB 1654.53 In stock
RMB 974.11 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Volasertib (BI 6727) has been cited by 89 publications

Purity & Quality Control

Choose Selective PLK Inhibitors

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.
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 MmPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXS3NkBp M{nVemlEPTB;MUewxtE2OSCwTR?= NYjRZlltOjV3N{[wO|Q>
KG-1 NVjV[JJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPhO|IhcA>? MlfsTWM2OD1zNUFCtVY4KG6P Ml32NlU2PzZyN{S=
MOLM-13 M1i4T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PBXlczKGh? NEXQ[2RKSzVyPUW3xtE1PCCwTR?= M2HwUFI2PTd4MEe0
MV-4-11 MlXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYO3NkBp NXr5e3lKUUN3ME2xOuKyPiCwTR?= NWWxb4pDOjV3N{[wO|Q>
NOMO-1 MmWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFn1Z204OiCq M3HNVGlEPTB;MUS1xtE4KG6P MWKyOVU4PjB5NB?=
OCI-AML3 NYrsO4NzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHoO|IhcA>? M3PVdWlEPTB;OUFCtVUyKG6P M4\0TlI2PTd4MEe0
SKM-1 MnqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHrO|IhcA>? MmnGTWM2OD17NdMxOVIhdk1? M4PNN|I2PTd4MEe0
THP-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrEZ3A4OiCq NX;G[WNmUUN3ME21OuKyOzlibl2= MoLKNlU2PzZyN{S=
MCF7/LTED  MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXpNJhLOi53LUSwJI5O NWG2Xot3PSCm MUXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NV3tOJF[OjV2OEC5OFM>
HCC1428/LTED M2iySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\peVIvPS12MDDuUS=> NGPMfY42KGR? MV7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1HOR|I2PDhyOUSz
A431 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWqwMVMxKG6P MXmxMVQh\A>? NVXEWXF4cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCCmb4PlMUBidmRidHnt[U1l\XCnbnTlcpQhdWGwbnXy NIPmc3ozOzh7MUC5Oi=>
FaDu  NVHVNW5MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXIOogxNTFyMECgcm0> M2n0cFEuPCCm NHrKcYpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NFPkSJkzOzh7MUC5Oi=>
SF188 M4DTXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUO1NE0yPTBibl2= NGXvdGk4OiCq MkfpSG1UVw>? NXP2cIxCcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M{L4WlI{QDh5NkS1
T98G NEPrdlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{L0clUxNTF3MDDuUS=> NILa[GQ4OiCq NVzjPFFJTE2VTx?= M1ywXYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> Ml;aNlM5QDd4NEW=
DU145 M2DUUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvjfFY1OTBxNUCvNlUxKG6P NF7iVpkzPCCq M33YVmlEPTB:MUCgcm0> MkW5NlM5QDR2Mki=
LNCaP M{\VPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVr0UIZMOTBxNUCvNlUxKG6P NYf2[4VtOjRiaB?= MVvJR|UxRDFyIH7N MYSyN|g5PDR{OB?=
PC3 NFOyW4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTnXpIyOC93MD:yOVAhdk1? M1LEOVI1KGh? M3\TOGlEPTEkiMy2NFAhdk1? NG\BO5EzOzh6NESyPC=>
RT4 NYrDR|RkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjs[2lyPDhiaB?= NXLNUo9UUUN3ME2xNVEvOjdibl2= NUD6ZZg1OjN5OUK2N|k>
5637 NGT5SG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHX2NHk1QCCq NHfRT25KSzVyPUGxOlUvOTRibl2= M13DUFI{Pzl{NkO5
T24 NHfI[FRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\DOFghcA>? NGf1[HJKSzVyPUKwOE46OSCwTR?= NWTQVHg{OjN5OUK2N|k>
KMCH-1 MUHBdI9xfG:|aYOgRZN{[Xl? MX6yNFAhdk1? NIXnT|kzPCCq M1zHTYlv\HWlZYOgZZBweHSxc3nz M3jWdFI{PzB|Nkez
Mz-ChA-1 MkLuRZBweHSxc3nzJGF{e2G7 NV3aOph5OjByIH7N NXHOdJEzOjRiaB?= Mmj2bY5lfWOnczDhdI9xfG:|aYO= M4G1bFI{PzB|Nkez
HUCCT-1 NYiwWoplSXCxcITvd4l{KEG|c3H5 NVz0R2hVOjByIH7N MlfHNlQhcA>? NHfRcVlqdmS3Y3XzJIFxd3C2b4Ppdy=> M4TCVlI{PzB|Nkez
HCT 116 M3PpN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjlNW5GSzVywrC9JFI{KG6P M1mxT|E6Ozh|OEKz
NCI-H460 M1frXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF36N4pGSzVywrC9JFIyKG6P M1XqdFE6Ozh|OEKz
HL-60 NEfhOYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLxXIRvTUN3MNMgQUA{OiCwTR?= MWixPVM5Ozh{Mx?=
THP-1 NVjKZW5XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF60[opGSzVyIE2gN|Yhdk1? MX[xPVM5Ozh{Mx?=
Raji NH;EdIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPGdYZLTUN3MDC9JFM4KG6P NFviWXgyQTN6M{iyNy=>

... Click to View More Cell Line Experimental Data

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
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.

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. 

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]


Kinase Assay:[1]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • 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.

* 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


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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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.

PLK Signaling Pathway Map

PLK Inhibitors with Unique Features

Related PLK Products

Tags: buy Volasertib (BI 6727) | Volasertib (BI 6727) supplier | purchase Volasertib (BI 6727) | Volasertib (BI 6727) cost | Volasertib (BI 6727) manufacturer | order Volasertib (BI 6727) | Volasertib (BI 6727) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID