BI 2536 is a novel, highly selective, potent inhibitor of Polo-like kinase 1 (Plk1) with an IC50 of 0.83 nM. BI 2536 has demonstrated favorable tolerability and antitumor activity in Phase I trials.
Oncogene. 2018 Mar 22.
HIPK2 and extrachromosomal histone H2B are separately recruited by Aurora-B for cytokinesis
BI 2536 purchased from AbMole
|Source||Oncogene (2018). Figure 2. Bi 2536 (AbMole BioScience)|
|Method||The kinase activity assay|
|Cell Lines||HeLa cells|
|Incubation Time||20 min|
|Results||To avoid earlystage effects on central spindle formation, PLK1 and Aurora-B were inhibited by BI 2536 and Hesperadin, respectively, in temporally controlled modes.|
|Cell lines||HeLa, A43, SKOV-3, HT-29, K562, A549, Saos-2, MCF7, HCT116, COLO 205, Hep G2, Raji and PC-3 cells line|
|Preparation method||cell viability were quantified by Alamar Blue assay, 72 hr after initiation of BI 2536 treatment or the vehicle control. The bar chart summarizes the mean values for half-maximal growth inhibition for each cell line (EC50 values; [nM]) on a logarithmic scale.|
|Incubation time||72 hr|
|Animal models||Nude mice bearing established HCT 116 tumors xenograft model|
|Dosages||50mg/kg once or twice weekly|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Reduced efficacy of the Plk1 inhibitor BI 2536 on the progression of hepatocellular carcinoma due to low intratumoral drug levels.
Haupenthal et al. Neoplasia. 2012 May;14(5):410-9. PMID: 22745587.
A randomised phase II trial of the Polo-like kinase inhibitor BI 2536 in chemo-naïve patients with unresectable exocrine adenocarcinoma of the pancreas - a study within the Central European Society Anticancer Drug Research (CESAR) collaborative network.
Mross et al. Br J Cancer. 2012 Jul 10;107(2):280-6. PMID: 22699824.
A Phase I Open-Label Dose-Escalation Study of Intravenous BI 2536 Together With Pemetrexed in Previously Treated Patients With Non-Small-Cell Lung Cancer.
Ellis et al. Clin Lung Cancer. 2012 May 31. PMID: 22658814.
In vitro PLK1 inhibition by BI 2536 decreases proliferation and induces cell-cycle arrest in melanoma cells.
de Oliveira et al. J Drugs Dermatol. 2012 May;11(5):587-92. PMID: 22527426.
Phase i study of the Plk1 inhibitor BI 2536 administered intravenously on three consecutive days in advanced solid tumours.
Frost et al. Curr Oncol. 2012 Feb;19(1):e28-35. PMID: 22328845.
Antiproliferative in vitro effects of BI 2536-mediated PLK1 inhibition on cervical adenocarcinoma cells.
Pezuk et al. Clin Exp Med. 2011 Nov 12. PMID: 22080235.
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