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BI6727 (Volasertib)

Catalog No.
A8558
Plk inhibitor,highly potent
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$110.00
In stock
5mg
$97.00
In stock
10mg
$174.00
In stock
50mg
$532.00
In stock
100mg
$871.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

BI6727 (Volasertib; CAS 755038-65-4) is a selective inhibitor of Polo-like kinases (Plk), primarily targeting Plk1 with an IC50 of 0.87 nM, and showing lower potency towards Plk2 (IC50 = 5 nM) and Plk3 (IC50 = 56 nM). Plk1 regulates the G2/M cell cycle transition and is commonly overexpressed in various tumor types, representing a potential therapeutic target. BI6727 inhibits proliferation across multiple tumor cell lines including colorectal (HCT116, EC50 = 23 nM), lung (NCI-H460, EC50 = 21 nM), melanoma (BRO, EC50 = 11 nM), and hematologic cancer (GRANTA, EC50 = 15 nM). In vivo, BI6727 administration induced apoptosis and reduced tumor growth in mouse HCT116 and NCI-H460 xenograft models.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt618.83
Cas No.755038-65-4
FormulaC34H50N8O3
SynonymsBI 6727; BI-6727
Solubilityinsoluble in H2O; ≥10.31 mg/mL in DMSO; ≥56.1 mg/mL in EtOH
Chemical NameN-[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
SDFDownload SDF
Canonical SMILESCCC1C(=O)N(C2=CN=C(N=C2N1C(C)C)NC3=C(C=C(C=C3)C(=O)NC4CCC(CC4)N5CCN(CC5)CC6CC6)OC)C
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

Human melanoma A375 and Hs 294T cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

24 h, 10-100 nM

Applications

BI6727 (Volasertib) is a second generation small molecule Plk1 inhibitor and has been reported to be a promising agent for treatment of several cancers. BI6727 (Volasertib) inhibits growth, viability and induces apoptosis of melanoma cells.

Clinical experiment [2]:

Animal models

Patients aged ≥ 18 years with locally advanced or metastatic urothelial cancer

Dosage form

BI6727 (Volasertib) was administered by 2-hour intravenous infusion at a dose of 300 mg once daily on day 1 of 3-week treatment cycles.

Application

BI6727 (Volasertib) has an acceptable safety profile as a second-line treatment for advanced or metastatic urothelial cancer, but only modest antitumor activity for further evaluation as a monotherapy.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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]. Stadler W M, Vaughn D J, Sonpavde G, et al. An open‐label, single‐arm, phase 2 trial of the polo‐like kinase inhibitor volasertib (BI 6727) in patients with locally advanced or metastatic urothelial cancer[J]. Cancer, 2014, 120(7): 976-982.

Biological Activity

Description BI6727 is a high potent inhibitor of Polo-like kinase with IC50 value of 0.87 nM.
Targets Polo-like kinase          
IC50 0.87 nM          

Quality Control