Volasertib (Synonyms: BI 6727)

Name: Volasertib
Brand: MedChemExpress
SKU: HY-12137
Rating: 5.0 (25 reviews)

Cat. No.: HY-12137 Purity: 99.41%: FAQs
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Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC₅₀ of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC₅₀s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models.

For research use only. We do not sell to patients.

Volasertib Chemical Structure

CAS No. : 755038-65-4

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 25 publication(s) in Google Scholar

Other Forms of Volasertib:

Volasertib trihydrochloride Get quote

24 Publications Citing Use of MCE Volasertib

Proliferation Assay

: Volasertib purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2017;43(4):1472-1486. [Abstract]; The addition of Volasertib (0.5-1.5 µg/mL blunts the increase of the percentage of annexin-V-binding erythrocytes following glucose deprivation, an effect reaching statistical significance at 1 and 1.5 µg/mL Volasertib.

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PLK1 PLK2 PLK3 PLK4

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[3]

PLK1

0.87 nM (IC₅₀)

PLK2

5 nM (IC₅₀)

PLK3

56 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	4137 nM Compound: 3; BI 6727	Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
A-427	IC₅₀	91 nM Compound: 44	Antiproliferative activity against human A-427 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay Antiproliferative activity against human A-427 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay	[PMID: 37197456]
A549	IC₅₀	0.08 μM Compound: BI6727; I	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
A549	IC₅₀	206.4 nM Compound: 3; BI 6727	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
DU-145	IC₅₀	< 4 nM Compound: 3; BI 6727	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
HCT-116	IC₅₀	0.11 μM Compound: BI6727; I	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
HCT-116	IC₅₀	602.4 nM Compound: 3; BI 6727	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
HEK-293T	IC₅₀	1.1 nM Compound: Volasertib	Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
HepG2	IC₅₀	< 4 nM Compound: 3; BI 6727	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
HT-29	IC₅₀	1133 nM Compound: 3; BI 6727	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
JeKo-1	IC₅₀	< 4 nM Compound: 3; BI 6727	Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
K562	IC₅₀	< 4 nM Compound: 3; BI 6727	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
KARPAS-299	IC₅₀	< 4 nM Compound: 3; BI 6727	Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
L02	IC₅₀	< 4 nM Compound: 3; BI 6727	Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
MCF7	IC₅₀	0.09 μM Compound: BI6727; I	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
MDA-MB-231	IC₅₀	0.11 μM Compound: BI6727; I	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
MDA-MB-231	IC₅₀	1482 nM Compound: 3; BI 6727	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]
MM1.S	IC₅₀	4.5 nM Compound: Volasertib	Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
NCI-H23	IC₅₀	53 nM Compound: 44	Antiproliferative activity against human NCI-H23 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay Antiproliferative activity against human NCI-H23 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay	[PMID: 37197456]
PC-3	IC₅₀	0.09 μM Compound: BI6727; I	Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30572179]
SMMC-7721	IC₅₀	77.2 nM Compound: 3; BI 6727	Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay	[PMID: 32814244]

In Vitro

Volasertib (BI 6727; 0.01-10000 nM; 72 hours) has EC₅₀ values of 11 to 37 nmol/L in multiple cell lines^[1].
Volasertib (10-1000 nM; 24 hours) results accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase^[1].
Volasertib (100 nM; 24-72 hours) induces cell apoptosis at 48 hours^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	Multiple cell lines
Concentration:	0.01-10000 nM
Incubation Time:	72 hours
Result:	Inhibited proliferation of multiple cell lines derived from various cancer tissues, including carcinomas of the colon (HCT 116, EC₅₀=23 nmol/L) and lung (NCI-H460, EC₅₀=21 nmol/L), melanoma (BRO, EC₅₀=11 nmol/L), and hematopoietic cancers (GRANTA-519, EC₅₀=15 nmol/L; HL-60, EC₅₀=32 nmol/L; THP-1, E₅₀=36 nmol/L and Raji, EC₅₀=37 nmol/L) with EC₅₀ values of 11 to 37 nmol/L.

Apoptosis Analysis^[1]

Cell Line:	NCI-H460 cells
Concentration:	100 nM
Incubation Time:	24, 48, 72 hours
Result:	G2-M arrest at 24 hours was followed by induction of apoptosis at 48 hours.

Cell Cycle Analysis^[1]

Cell Line:	NCI-H460 cells
Concentration:	10, 30, 100, 300, 1000 nM
Incubation Time:	24 hours
Result:	Resulted in accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase.

In Vivo

Volasertib (BI 6727; A total weekly dose of 50 mg/kg; Oral; once a week, twice a week, or daily; for 40 days) shows comparable efficacy in human colon carcinoma xenograft models^[1].
Volasertib (15, 20, or 25 mg/kg/day; i.v.; 2 consecutive days per week; for 40 days) leads to significant tumor growth delay and even tumor regression in human colon carcinoma xenograft models ^[1].
Volasertib (70 mg/kg given once weekly or 10 mg/kg daily; oral) significantly delays tumor growth in a non-small cell lung carcinoma xenograft model derived from NCI-H460 cells^[1].
Volasertib (a single dose of 40 mg/kg; iv) causes a significant (13-fold) increase in mitotic cells in HCT 116 tumor-bearing nude mice^[1].
Volasertib has high volume of distribution and a long terminal half-life in mice (V_ss=7.6 L/kg, t_1/2=46 h) and rats (V_ss=22 L/kg, t_1/2=54 h)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BomTac:NMRI-Foxn1^nu mice (Taconic) were grafted s.c. with HCT 116 human colon carcinoma cells (ATCC CCL-247)^[1]
Dosage:	A total weekly dose of 50 mg/kg
Administration:	Oral; once a week, twice a week, or daily; for 40 days
Result:	Showed comparable efficacy and were well tolerated.

Animal Model:	Female BomTac:NMRI-Foxn1^nu mice and male Wistar rats of the strain Crl:WI^[1]
Dosage:	35 mg/kg (mice) or 10 mg/kg (rat) (Pharmacokinetic Analysis)
Administration:	IV 5-minute infusion; a single dose 5-minute infusion
Result:	Had high volume of distribution and a long terminal half-life in mice (V_ss=7.6 L/kg, t_1/2=46 h) and rats (V_ss=22 L/kg, t_1/2=54 h).

Clinical Trial

Molecular Weight

618.81

Formula

C₃₄H₅₀N₈O₃

CAS No.

755038-65-4

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC=C(C(OC)=C1)NC2=NC=C(N(C3=O)C)C(N([C@@H]3CC)C(C)C)=N2)N[C@H]4CC[C@@H](CC4)N5CCN(CC5)CC6CC6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (40.40 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6160 mL	8.0800 mL	16.1600 mL
5 mM	0.3232 mL	1.6160 mL	3.2320 mL
10 mM	0.1616 mL	0.8080 mL	1.6160 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.36 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.41%

Select Batch:

Data Sheet (277 KB) SDS (392 KB)

COA (245 KB) LCMS (100 KB)

Handling Instructions (2659 KB)

References

[1]. Xie FF, et al. Volasertib suppresses tumor growth in cervical cancer. Am J Cancer Res. 2015 Nov 15;5(12):3548-59. [Content Brief]

[2]. Rudolph D, et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity.Clin Cancer Res. 2009 May 1;15(9):3094-102. Epub [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6160 mL	8.0800 mL	16.1600 mL	40.4001 mL
	5 mM	0.3232 mL	1.6160 mL	3.2320 mL	8.0800 mL
	10 mM	0.1616 mL	0.8080 mL	1.6160 mL	4.0400 mL
	15 mM	0.1077 mL	0.5387 mL	1.0773 mL	2.6933 mL
	20 mM	0.0808 mL	0.4040 mL	0.8080 mL	2.0200 mL
	25 mM	0.0646 mL	0.3232 mL	0.6464 mL	1.6160 mL
	30 mM	0.0539 mL	0.2693 mL	0.5387 mL	1.3467 mL
	40 mM	0.0404 mL	0.2020 mL	0.4040 mL	1.0100 mL

Volasertib Related Classifications

Help & FAQs

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Volasertib (Synonyms: BI 6727)

Customer Review

Other Forms of Volasertib:

24 Publications Citing Use of MCE Volasertib

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Volasertib (Synonyms: BI 6727)

Customer Review

Other Forms of Volasertib:

Volasertib Related Antibodies

24 Publications Citing Use of MCE Volasertib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Polo-like Kinase (PLK) Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Volasertib Related Antibodies

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Complete Stock Solution Preparation Table

Volasertib Related Classifications

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