Name: Volasertib (BI6727)
Brand: Selleck Chemicals
SKU: S2235
Availability: InStock
Rating: 5 (176 reviews)

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Quality Control

Batch: Purity: 99.78%

99.78

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase
Other PLK Inhibitors	BI 2536 Rigosertib (ON-01910) GSK461364 Onvansertib (NMS-1286937, NMS-P937) CFI-400945 Ro3280 HMN-214 SBE 13 HCl Centrinone (LCR-263) MLN0905

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
KASUMI-1	Growth Inhibition Assay		72 h		IC50=170±51 nM	25576074
KG-1	Growth Inhibition Assay		72 h		IC50=150±67 nM	25576074
MOLM-13	Growth Inhibition Assay		72 h		IC50=57±44 nM	25576074
MV-4-11	Growth Inhibition Assay		72 h		IC50=16±6 nM	25576074
NOMO-1	Growth Inhibition Assay		72 h		IC50=145±7 nM	25576074
OCI-AML3	Growth Inhibition Assay		72 h		IC50=90±51 nM	25576074
SKM-1	Growth Inhibition Assay		72 h		IC50=95±52 nM	25576074
THP-1	Growth Inhibition Assay		72 h		IC50=56±39 nM	25576074
MCF7/LTED	Growth Inhibition Assay	2.5-40 nM	5 d		inhibits cell growth in a dose-dependent manner	25480943
HCC1428/LTED	Growth Inhibition Assay	2.5-40 nM	5 d		inhibits cell growth in a dose-dependent manner	25480943
A431	Growth Inhibition Assay	0-30 nM	1-4 d		inhibits cell growth in both dose- and time-dependent manner	23891096
FaDu	Growth Inhibition Assay	0-1000 nM	1-4 d		inhibits cell growth in both dose- and time-dependent manner	23891096
SF188	Growth Inhibition Assay	50-150 nM	72 h	DMSO	inhibits cell proliferation	23887645
T98G	Growth Inhibition Assay	50-150 nM	72 h	DMSO	inhibits cell proliferation	23887645
DU145	Growth Inhibition Assay	10/50/250 nM	24 h		IC50<10 nM	23884428
LNCaP	Growth Inhibition Assay	10/50/250 nM	24 h		IC50<10 nM	23884428
PC3	Growth Inhibition Assay	10/50/250 nM	24 h		IC50∼600 nM	23884428
RT4	Growth Inhibition Assay		48 h		IC50=111.27 nM	23792639
5637	Growth Inhibition Assay		48 h		IC50=1165.14 nM	23792639
T24	Growth Inhibition Assay		48 h		IC50=204.91 nM	23792639
KMCH-1	Apoptosis Assay	200 nM	24 h		induces apoptosis	23703673
Mz-ChA-1	Apoptosis Assay	200 nM	24 h		induces apoptosis	23703673
HUCCT-1	Apoptosis Assay	200 nM	24 h		induces apoptosis	23703673
HCT 116	Growth Inhibition Assay				EC50 = 23 nM	19383823
NCI-H460	Growth Inhibition Assay				EC50 = 21 nM	19383823
BRO	Growth Inhibition Assay				EC50 = 11 nM	19383823
GRANTA-519	Growth Inhibition Assay				EC50 = 15 nM	19383823
HL-60	Growth Inhibition Assay				EC50 = 32 nM	19383823
THP-1	Growth Inhibition Assay				EC50 = 36 nM	19383823
Raji	Growth Inhibition Assay				EC50 = 37 nM	19383823
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
Rh30	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
SKBR3	Cytotoxicity assay		24 hrs		Cytotoxicity against human SKBR3 cells after 24 hrs by MTT assay	29288948
MDA-MB-231	Cytotoxicity assay		24 hrs		Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay	29288948
MDA-MB-468	Cytotoxicity assay		24 hrs		Cytotoxicity against human MDA-MB-468 cells after 24 hrs by MTT assay	29288948
BT474	Cytotoxicity assay		24 hrs		Cytotoxicity against human BT474 cells after 24 hrs by MTT assay	29288948
ZR-75-1	Cytotoxicity assay		24 hrs		Cytotoxicity against human ZR-75-1 cells after 24 hrs by MTT assay	29288948
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 35 mg/mL (56.56 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	4%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (3.23mM)	Taking the 1 mL working solution as an example, add 40 μL of 50 mg/ml clear DMSO stock solution to 960 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.150mg/ml (1.86mM)	Taking the 1 mL working solution as an example, add 50 μL of 23 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	618.81	Formula	C₃₄H₅₀N₈O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	755038-65-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BI 6727			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

Mechanism of Action

Features	A high volume of distribution, indicating good tissue penetration, and a long terminal half-life.
Targets/IC₅₀/Ki	PLK1 (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, this compound also potently inhibits two closely related kinases Plk2 and Plk3 with IC50 of 5 nM and 56 nM, respectively. This chemical at concentrations up to 10 μM displays no inhibitory activity against a panel of >50 other kinases. It 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. This compound 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. Low nanomolar concentrations of this inhibitor display potent inhibitory activity against neuroblastoma (NB) tumor-initiating cells (NB TIC) with EC50 of 21 nM, whereas only micromolar concentrations of it are cytotoxic for normal pediatric neural stem cells. It induces growth arrest of Daoy and ONS-76 medulloblastoma cells similar to BI 2536.
Kinase Assay	In vitro kinase assays
Kinase Assay	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 this compound 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.
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. In in vivo studies, this compound shows better toxicity and pharmacokinetic profile compared to BI2536.
References	[1] https://pubmed.ncbi.nlm.nih.gov/19383823/ [2] https://pubmed.ncbi.nlm.nih.gov/21303981/ [3] https://pubmed.ncbi.nlm.nih.gov/22390279/

Applications

Methods	Biomarkers	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
Immunofluorescence	PLK1 / Wee1	29108241
Growth inhibition assay	Cell viability	29383095

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02722135	Withdrawn	Leukemia Myeloid Acute	Boehringer Ingelheim	November 2016	Phase 1
NCT02721875	Terminated	Myelodysplastic Syndromes	Boehringer Ingelheim	April 28 2016	Phase 1
NCT02201329	Completed	Myelodysplastic Syndromes\|Leukemia Myelomonocytic Chronic	Boehringer Ingelheim	August 2014	Phase 1
NCT01971476	Completed	Leukemia\|Neoplasms	Boehringer Ingelheim	October 22 2013	Phase 1
NCT01772563	Completed	Neoplasms	Boehringer Ingelheim	February 4 2013	Phase 1
NCT01662505	Completed	Leukemia Myeloid Acute	Boehringer Ingelheim	August 2012	Phase 1

Tech Support

Handling Instructions

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

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

Frequently Asked Questions

Question 1:
I wonder how to reconstitute it for in vivo studies?

Answer:
It can be dissolved in 4% DMSO+Corn oil at 2mg/ml for i.p. injection in mice. For oral administration, this compound 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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Volasertib (BI6727) PLK1 inhibitor

Chemical Structure

Molecular Weight: 618.81