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BI 2536

In stock
Catalog No.
A3965
Plk1 inhibitor,potent and ATP-competitive
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$125.00
In stock
Evaluation Sample
$28.00
In stock
5mg
$85.00
In stock
10mg
$150.00
In stock
50mg
$470.00
In stock

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Background

BI 2536 is a potent, ATP-competitive, well tolerated and highly specific human polo-like kinase 1 (PLK1) inhibitor with IC value of 0.83 nM, which shows 1000-fold selectivity against other kinases [1].

BI 2536 has been demonstrated to suppress cell growth and colony formation, it has been shown to induce mitotic arrest at G2/M phase and apoptosis in human cervical adenocarcinoma cell line HeLa [2].

BI 2536 has shown to have the effect of inhibiting cell proliferation in more than 20 tumor cell lines with half maximal effective concentration (EC50) values ranging from 2–25 nM. In vivo, multiple studies in xenograft models of human carcinoma have shown the anti-tumor activity of BI 2536 when the drug was intravenously administered 1-2 times every week [1].

References:
[1] Schöffski P. Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology. Oncologist. 2009 Jun;14(6):559-70.
[2] Pezuk JA1, Brassesco MS, Oliveira JC, Morales AG, Montaldi AP, Sakamoto-Hojo ET, Scrideli CA, Tone LG. Antiproliferative in vitro effects of BI 2536-mediated PLK1 inhibition on cervical adenocarcinoma cells. Clin Exp Med. 2013 Feb;13(1):75-80.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt521.67
Cas No.755038-02-9
FormulaC28H39N7O3
SynonymsBI-2536;BI2536
Solubility≥13.04 mg/mL in DMSO, ≥92.4 mg/mL in EtOH with ultrasonic, <2.56 mg/mL in H2O
Chemical Name4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
SDFDownload SDF
Canonical SMILESCCC1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment: [1]

Cell lines

HeLa-S3 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 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

1 μM, 24 hours

Applications

The effect of BI 2536 on the cell-cycle profile of cancer cells grown in vitro was assessed by immunofluorescence microscopy and flow cytometry. BI2536 caused HeLa cells to accumulate with a 4N DNA content, indicative of a cell-cycle block in either G2 phase or mitosis. The mitotic figures observed in BI 2536-treated cultures of HeLa cells displayed abnormal mitotic figures at EC50 values closely matching the induction of a G2/M arrest.

Animal experiment: [1]

Animal models

Immunodeficient nu/nu mice injected with HCT 116 cells

Dosage form

Intravenous injection, 40–50mg/kg, once or twice per week

Applications

The administration of BI 2536 was found to be highly efficacious in diverse xenograft models, such as the HCT 116 colon cancer with complete tumor suppression with the twice per week schedule and a T/C value of 16% with once per week treatment. By using a more rigorous model of larger HCT 116 tumors, in which treatment was delayed until cancer nodules reached a median size of 500 mm3, it was found that five cycles of BI 2536 induced marked tumor regressions, whereas the control mice showed progressive disease.

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] Steegmaier M, Hoffmann M, Baum A, et al. BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo. Current Biology, 2007, 17(4): 316-322.

Biological Activity

Description BI2536 is a potent inhibitor of Plk1 with IC50 of 0.83 nM.
Targets Plk1          
IC50 0.83 nM          

Quality Control

Chemical structure

BI 2536

Related Biological Data

BI 2536

Related Biological Data

BI 2536

Related Biological Data

BI 2536