Volasertib trihydrochloride
Based on 38 publication(s) in Google Scholar
Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models.
For research use only. We do not sell to patients.
- Purity: 99.12%
- CAS No.: 946161-17-7
- Formula: C34H53Cl3N8O3
- Molecular Weight:728.20
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Volasertib trihydrochloride
More- Cell. 2025 Jun 26;188(13):3405-3421.e27. [Abstract]
- Nat Commun. 2024 Mar 16;15(1):2377. [Abstract]
- Nat Commun. 2020 Aug 13;11(1):4053. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Theranostics. 2024 May 19;14(8):3104-3126. [Abstract]
- Cell Discov. 2022 Sep 14;8(1):92. [Abstract]
- J Colloid Interface Sci. 2025 Jun 9;699(Pt 1):138144. [Abstract]
- NPJ Precis Oncol. 2025 Nov 21;9(1):373. [Abstract]
- PLoS Biol. 2025 Nov 24;23(11):e3003490. [Abstract]
- Cell Death Discov. 2025 Mar 4;11(1):86. [Abstract]
- Sci Signal. 2025 Mar 18;18(878):eadi5174. [Abstract]
- Mol Cancer Ther. 2024 Oct 1;23(10):1404-1417. [Abstract]
- Pharmaceutics. 2022 Jun 6;14(6):1209. [Abstract]
- Mol Cancer Ther. 2018 Apr;17(4):825-837. [Abstract]
- Bioorg Chem. 2022 Feb:119:105505. [Abstract]
- Spectrochim Acta A Mol Biomol Spectrosc. 2024 Jul 15:322:124823. [Abstract]
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Feb 10;1870(4):167062. [Abstract]
- J Inflamm Res. 2025 Mar 25:18:4381-4394. [Abstract]
- Sci Rep. 2017 Sep 8;7(1):11026. [Abstract]
- PLoS Genet. 2023 Aug 28;19(8):e1010903. [Abstract]
- J Photochem Photobiol B. 2022 Jul:232:112477. [Abstract]
- Biochim Biophys Acta. 2018 May;1862(5):1134-1147. [Abstract]
- Med Oncol. 2025 Jul 21;42(8):358. [Abstract]
- PLoS Negl Trop Dis. 2016 Jan 11;10(1):e0004356. [Abstract]
- Dis Model Mech. 2023 Mar 1;16(3):dmm049769. [Abstract]
- J Cancer. 2024 Mar 4;15(8):2318-2328. [Abstract]
- Oncol Lett. 2024 May 14;28(1):316. [Abstract]
- Arch Oral Biol. 2026 May:185:106557. [Abstract]
- Connect Tissue Res. 2025 May 21:1-24. [Abstract]
- Cell Physiol Biochem. 2017;43(4):1472-1486. [Abstract]
- Vet Comp Oncol. 2026 Apr 26. [Abstract]
- bioRxiv. 2026 May 29.
- Res Sq. 2026 Apr 28.
- bioRxiv. 2026 Jan 27.
- Chemrxiv. 2024 Feb 8.
- Oncotarget. 2018 Sep 11;9(71):33482-33499. [Abstract]
- University of California. 2016.
Customer Validation & Images
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In Vivo Efficacy Study
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WB
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WB
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
Biological Activity
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PLK1 0.87 nM (IC50) |
PLK2 5 nM (IC50) |
PLK3 56 nM (IC50) |
Volasertib trihydrochloride (BI 6727 trihydrochloride; 0.01-10000 nM; 72 hours) has EC50 values of 11 to 37 nmol/L in multiple cell lines[1].
Volasertib trihydrochloride (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 trihydrochloride (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.
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Cell Line:Multiple cell lines
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Concentration:0.01-10000 nM
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Incubation Time:72 hours
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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.
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Cell Line:NCI-H460 cells
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Concentration:100 nM
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Incubation Time:24, 48, 72 hours
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Result:G2-M arrest at 24 hours was followed by induction of apoptosis at 48 hours.
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Cell Line:NCI-H460 cells
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Concentration:10, 30, 100, 300, 1000 nM
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Incubation Time:24 hours
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Result:Resulted in accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase.
Volasertib trihydrochloride (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 trihydrochloride (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 (Vss=7.6 L/kg, t1/2=46 h) and rats (Vss=22 L/kg, t1/2=54 h)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BomTac:NMRI-Foxn1nu mice (Taconic) were grafted s.c. with HCT 116 human colon carcinoma cells (ATCC CCL-247)[1]
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Dosage:A total weekly dose of 50 mg/kg
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Administration:Oral; once a week, twice a week, or daily; for 40 days
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Result:Showed comparable efficacy and were well tolerated.
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Animal Model:Female BomTac:NMRI-Foxn1nu mice and male Wistar rats of the strain Crl:WI[1]
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Dosage:35 mg/kg (mice) or 10 mg/kg (rat) (Pharmacokinetic Analysis)
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Administration:IV 5-minute infusion; a single dose 5-minute infusion
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Result:Had high volume of distribution and a long terminal half-life in mice (Vss=7.6 L/kg, t1/2=46 h) and rats (Vss=22 L/kg, t1/2=54 h).
Chemical Information
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CAS No. 946161-17-7
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Appearance Solid
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Molecular Weight 728.20
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Formula C34H53Cl3N8O3
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Color Off-white to light yellow
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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.[H]Cl.[H]Cl.[H]Cl
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Synonyms
BI 6727 trihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (38)
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Journal Impact Factor
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Most Recent
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Cell
Extrachromosomal DNA replication and maintenance couple with DNA damage pathway in tumors. [Abstract]2025 Jun 26;188(13):3405-3421.e27. PMID: 40300601 -
Nat Commun
2024 Mar 16;15(1):2377. PMID: 38493213
Volasertib trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Mar 16;15(1):2377. [Abstract]
Immunoblot of NUDT1 p-S121 in Kelly cells treated with PLK1 shRNA or BI6727 (20 nM, 0, 24, 48 h).
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Nat Commun
PLK1 inhibition exhibits strong anti-tumoral activity in CCND1-driven breast cancer metastases with acquired palbociclib resistance. [Abstract]2020 Aug 13;11(1):4053. PMID: 32792481 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Theranostics
Single-cell analyses reveal evolution mimicry during the specification of breast cancer subtype. [Abstract]2024 May 19;14(8):3104-3126. PMID: 38855191 -
Cell Discov
Single-cell profiling reveals molecular basis of malignant phenotypes and tumor microenvironments in small bowel adenocarcinomas. [Abstract]2022 Sep 14;8(1):92. PMID: 36104333
Volasertib trihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 14;8(1):92. [Abstract]
Cell survival curve for HUTU-80 cells treated with the indicated inhibitors with Volasertib from 0 to 100 μM (36 h).
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J Colloid Interface Sci
In situ generation of anti-leukemia vaccine by immunogenic dual-drug nanomedicine and polymersomal CpG nanoadjuvant. [Abstract]2025 Jun 9;699(Pt 1):138144. PMID: 40527143 -
NPJ Precis Oncol
Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]2025 Nov 21;9(1):373. PMID: 41272086
Volasertib trihydrochloride purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Nov 21;9(1):373. [Abstract]
MCL17-PDX mice were treated as indicated: vehicle (n = 5), abemaciclib (50 mg/kg, oral, daily; n = 5), and volasertib (5 mg/kg, intraperitoneal, weekly; n = 5). Tumor size was measured every 7 days during the treatment. Tumor volume = length x width2/2. Mice were euthanized after 21 days of treatment. Tumors were excised and weighed in comparison between each group.
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PLoS Biol
The cell cycle regulator PLK1 promotes murine melanoma progression by regulating the transcription factor BACH1. [Abstract]2025 Nov 24;23(11):e3003490. PMID: 41284701 -
Cell Death Discov
CeDaD-a novel assay for simultaneous tracking of cell death and division in a single population. [Abstract]2025 Mar 4;11(1):86. PMID: 40038265 -
Sci Signal
The kinase PLK1 promotes Hedgehog signaling-dependent resistance to the antiandrogen enzalutamide in metastatic prostate cancer. [Abstract]2025 Mar 18;18(878):eadi5174. PMID: 40100956
Volasertib trihydrochloride purchased from MedChemExpress. Usage Cited in: Sci Signal. 2025 Mar 18;18(878):eadi5174. [Abstract]
BI6727 (BI) treatment rescued the protein levels of PDCD4 resulting from nocodazole (Noc)–mediated mitotic arrest. DU145 shCtl and shPLK1 cells were generated with lentivirus expressing control shRNA or one of two specific PLK1 shRNA, followed by nocodazole (100 ng/ml) or 10 nM BI6727 treatment for 16 hours. The protein levels of PLK1 and PDCD4 were determined by immunoblotting, with β-actin and p-H3 as controls for loading and mitotic arrest. Blots are representative of three independent experiments
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Mol Cancer Ther
AKT Inhibition Sensitizes to Polo-Like Kinase 1 Inhibitor Onvansertib in Prostate Cancer. [Abstract]2024 Oct 1;23(10):1404-1417. PMID: 38894678 -
Pharmaceutics
Navitoclax Enhances the Therapeutic Effects of PLK1 Targeting on Lung Cancer Cells in 2D and 3D Culture Systems. [Abstract]2022 Jun 6;14(6):1209. PMID: 35745782 -
Mol Cancer Ther
Essential Role of Polo-like Kinase 1 (Plk1) Oncogene in Tumor Growth and Metastasis of Tamoxifen-Resistant Breast Cancer. [Abstract]2018 Apr;17(4):825-837. PMID: 29437878 -
Bioorg Chem
2022 Feb:119:105505. PMID: 34838332 -
Spectrochim Acta A Mol Biomol Spectrosc
Spectroscopic study on volasertib: Highly stable complexes with albumin and encapsulation into alginate/montmorillonite bionanocomposites. [Abstract]2024 Jul 15:322:124823. PMID: 39033609 -
J Cell Mol Med
2026 Apr;30(7):e71101. PMID: 41896195 -
Biochim Biophys Acta Mol Basis Dis
YAP/Aurora A-mediated ciliogenesis regulates ionizing radiation-induced senescence via Hedgehog pathway in tumor cells. [Abstract]2024 Feb 10;1870(4):167062. PMID: 38342416 -
J Inflamm Res
PLK1 Mediates the Proliferation and Contraction of Airway Smooth Muscle Cells and Has a Role in T2-High Asthma with Neutrophilic Inflammation Model. [Abstract]2025 Mar 25:18:4381-4394. PMID: 40162075 -
Sci Rep
Differential gene expression profiling linked to tumor progression of splenic marginal zone lymphoma. [Abstract]2017 Sep 8;7(1):11026. PMID: 28887496 -
PLoS Genet
Genetic enhancers of partial PLK1 inhibition reveal hypersensitivity to kinetochore perturbations. [Abstract]2023 Aug 28;19(8):e1010903. PMID: 37639469 -
J Photochem Photobiol B
Shedding light on the binding mechanism of kinase inhibitors BI-2536, Volasetib and Ro-3280 with their pharmacological target PLK1. [Abstract]2022 Jul:232:112477. PMID: 35644070 -
Biochim Biophys Acta
2018 May;1862(5):1134-1147. PMID: 29410075 -
Med Oncol
Ursolic acid affects autophagy and apoptosis of breast cancer through PLK1 via AKT/mTOR signaling pathway. [Abstract]2025 Jul 21;42(8):358. PMID: 40691672 -
PLoS Negl Trop Dis
Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (PLK1), a Potential Drug Target in Schistosoma mansoni. [Abstract]2016 Jan 11;10(1):e0004356. PMID: 26751972 -
Dis Model Mech
A Drosophila chemical screen reveals targeting MEK and DGKa mitigates Ras-driven polarity-impaired tumour growth. [Abstract]2023 Mar 1;16(3):dmm049769. PMID: 36861754 -
J Cancer
2024 Mar 4;15(8):2318-2328. PMID: 38495493 -
Oncol Lett
PLK1 inhibition leads to mitotic arrest and triggers apoptosis in cholangiocarcinoma cells. [Abstract]2024 May 14;28(1):316. PMID: 38807667 -
Arch Oral Biol
Construction of a DNA damage response-related signature for prognostication and therapeutic response prediction in head and neck squamous cell carcinoma. [Abstract]2026 May:185:106557. PMID: 41747404 -
Connect Tissue Res
Activation of the mechanosensitive ion channels TRPV4 and PIEZO1 downregulates key regulatory systems in the chondrocyte mechanome. [Abstract]2025 May 21:1-24. PMID: 40395084 -
Cell Physiol Biochem
2017;43(4):1472-1486. PMID: 29035889
Volasertib trihydrochloride 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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Vet Comp Oncol
Comparative Response of Canine and Human Osteosarcoma Tumour Cell Lines to Molecularly Targeted Anticancer Agents at Clinically Relevant Exposures With Analysis of Genomic Biomarkers. [Abstract]2026 Apr 26. PMID: 42036120 -
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Oncotarget
Generation and characteristics of a novel "double-hit" high grade B-cell lymphoma cell line DH-My6 with MYC/ IGH and BCL6/ IGH gene arrangements and potential molecular targeted therapies. [Abstract]2018 Sep 11;9(71):33482-33499. PMID: 30323893 -
Solvent & Solubility
H2O : ≥ 100 mg/mL (137.32 mM)
DMSO : 100 mg/mL (137.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.3732 mL | 6.8662 mL | 13.7325 mL | 34.3312 mL |
| 5 mM | 0.2746 mL | 1.3732 mL | 2.7465 mL | 6.8662 mL | |
| 10 mM | 0.1373 mL | 0.6866 mL | 1.3732 mL | 3.4331 mL | |
| 15 mM | 0.0915 mL | 0.4577 mL | 0.9155 mL | 2.2887 mL | |
| 20 mM | 0.0687 mL | 0.3433 mL | 0.6866 mL | 1.7166 mL | |
| 25 mM | 0.0549 mL | 0.2746 mL | 0.5493 mL | 1.3732 mL | |
| 30 mM | 0.0458 mL | 0.2289 mL | 0.4577 mL | 1.1444 mL | |
| 40 mM | 0.0343 mL | 0.1717 mL | 0.3433 mL | 0.8583 mL | |
| 50 mM | 0.0275 mL | 0.1373 mL | 0.2746 mL | 0.6866 mL | |
| 60 mM | 0.0229 mL | 0.1144 mL | 0.2289 mL | 0.5722 mL | |
| 80 mM | 0.0172 mL | 0.0858 mL | 0.1717 mL | 0.4291 mL | |
| 100 mM | 0.0137 mL | 0.0687 mL | 0.1373 mL | 0.3433 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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