GLPBio

BI6727(Volasertib)

Catalog No.: GC11224Purity:>99.00%Synonyms: BI 6727; BI-6727
COASDSData Sheet
BI6727(Volasertib) (BI 6727) ist ein oral aktiver, hochpotenter und ATP-kompetitiver Polo-like-Kinase-1 (PLK1)-Inhibitor mit einem IC50 von 0,87 nM. BI6727 (Volasertib) hemmt PLK2 und PLK3 mit IC50-Werten von 5 bzw. 56 nM. BI6727 (Volasertib) induziert mitotischen Arrest und Apoptose. BI6727 (Volasertib), ein Dihydropteridinon-Derivat, zeigt in mehreren Krebsmodellen eine ausgeprÄgte AntitumoraktivitÄt.

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BI6727(Volasertib)
Cas No.: 755038-65-4
10mM (in 1mL DMSO)In Stock
$78.00
1
1mgIn Stock
$24.00
1
5mgIn Stock
$57.00
1
10mgIn Stock
$91.00
1
25mgIn Stock
$191.00
1
50mgIn Stock
$263.00
1
100mgIn Stock
$364.00
1
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Zitate (Citations)

1 publicationsPublikationen von Forschern, die dieses Produkt verwenden

Beschreibung (Description)

BI6727(Volasertib) is an orally ATP-competitive polo-like kinase (PLK) inhibitor and potently inhibits PLK1, PLK2 and PLK3 with IC50 values of 0.87nM, 5nM and 56nM, respectively[1]. BI6727 has been widely used in various cancer cell lines and cancer xenograft models as an anti-cancer agent[2].

In vitro, BI6727 treatment for 4 days significantly inhibited the viability of anaplastic thyroid cancer (ATC) cell lines, with the IC50 values of 22.7nM for 8505C cells and 51.2nM for KAT18 cells, respectively[3]. Treatment of HeLa cells with 0.03μM BI6727 for 48 hours significantly inhibited cell growth, induced cell cycle arrest in G2/M phase, and cell apoptosis, and decreased the protein expression of PLK1 substrates survivin and wee1[4]. Treatment of A375 cells with 100nM BI6727 for 24h resulted in the decreased growth, viability, and colony-forming survival as well as increased apoptosis[5].

In vivo, BI6727 treatment (20mg/kg/week; i.p.) for 5 weeks significantly suppressed tumor volume and weight in the H526 cell xenograft mouse model without changing body weight[6]. Intravenous injection of BI6727 at a dose of 40mg/kg once weekly for 12 weeks significantly reduced tumor volume and prolonged mouse survival in MV-4-11 tumor-bearing nude mice[7].

References:
[1] Rudolph D, Steegmaier M, Hoffmann M, et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity[J]. Clinical cancer research, 2009, 15(9): 3094-3102.
[2] Gjertsen B T, Schöffski P. Discovery and development of the Polo-like kinase inhibitor volasertib in cancer therapy[J]. Leukemia, 2015, 29(1): 11-19.
[3] Lin S F, Yeh C N, Huang Y T, et al. Therapeutic inhibition of polo‐like kinases in anaplastic thyroid cancer[J]. Cancer Science, 2021, 112(2): 803-814.
[4] Xie F F, Pan S S, Ou R Y, et al. Volasertib suppresses tumor growth and potentiates the activity of cisplatin in cervical cancer[J]. American journal of cancer research, 2015, 5(12): 3548.
[5] Cholewa B D, Ndiaye M A, Huang W, et al. Small molecule inhibition of polo-like kinase 1 by volasertib (BI 6727) causes significant melanoma growth delay and regression in vivo[J]. Cancer letters, 2017, 385: 179-187.
[6] Zhang G, Pannucci A, Ivanov A A, et al. Polo-like Kinase 1 Inhibitors Demonstrate In Vitro and In Vivo Efficacy in Preclinical Models of Small Cell Lung Cancer[J]. Cancers, 2025, 17(3): 446.
[7] Rudolph D, Impagnatiello M A, Blaukopf C, et al. Efficacy and mechanism of action of volasertib, a potent and selective inhibitor of Polo-like kinases, in preclinical models of acute myeloid leukemia[J]. The Journal of pharmacology and experimental therapeutics, 2015, 352(3): 579-589.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

A375 cells

Preparation Method

A375 cells (1×105) were seeded in 6-well tissue culture dishes and treated with BI6727 (1, 10, 25, 50, and 100nM) for 24h. After treatment, the cells were trypsinized for 5min and then transferred to a 5mL centrifuge tube containing medium. The cells were centrifuged at 1000RPM for 2min, the supernatant was aspirated, and the cells were resuspended in 4% paraformaldehyde for fixation before flow cytometry analysis.

Reaction Conditions

1, 10, 25, 50, and 100nM; 24h

Applications

BI6727 significantly induced apoptosis of A375 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

Athymic (nu/nu) mice

Preparation Method

Six-week-old athymic (nu/nu) mice were housed in microisolation cages under pathogen-free conditions and fed laboratory food and water ad libitum. H526 cells (1×107) suspended in serum-free medium were mixed with Matrigel solution and injected subcutaneously into the flank region of mice. Subcutaneous tumor growth was measured until the tumor size reached approximately 100mm3. Tumor-bearing mice were matched by body weight and tumor volume and randomly assigned to each treatment group, with 6-8 mice in each group. Mice were treated with the following compounds: BI6727 (20mg/kg; weekly intraperitoneal injection), cisplatin (3mg/kg; weekly i.p.), irinotecan (25mg/kg; weekly i.p.), and cisplatin (3mg/kg; weekly i.p.). Tumor volume (V = 1/2ab2, where "a" and "b" represent tumor length and width, respectively) and body weight were monitored twice weekly. At the end of the experiment, subcutaneous tumors were removed and weighed.

Dosage form

20mg/kg/week; for 5 weeks; i.p.

Applications

BI6727 treatment significantly suppressed tumor volume and weight without changing the body weight of mice.

References:
[1] Cholewa B D, Ndiaye M A, Huang W, et al. Small molecule inhibition of polo-like kinase 1 by volasertib (BI 6727) causes significant melanoma growth delay and regression in vivo[J]. Cancer letters, 2017, 385: 179-187.
[2] Zhang G, Pannucci A, Ivanov A A, et al. Polo-like Kinase 1 Inhibitors Demonstrate In Vitro and In Vivo Efficacy in Preclinical Models of Small Cell Lung Cancer[J]. Cancers, 2025, 17(3): 446.

Produktdokumente (Product Documents)

Purity:>99.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
755038-65-4
Synonyme
BI 6727; BI-6727
Chemischer Name
N-[4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl]-4-[[(7R)-7-ethyl-5-methyl-6-oxo-8-propan-2-yl-7H-pteridin-2-yl]amino]-3-methoxybenzamide
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
Summenformel
C34H50N8O3
Molekulargewicht
618.83
Löslichkeit
≥ 10.3mg/mL in DMSO
Lagerung
4°C, protect from light
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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