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.
|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.
|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.|
Oncogene. 2018 Mar 22.
HIPK2 and extrachromosomal histone H2B are separately recruited by Aurora-B for cytokinesis
BI 2536 purchased from AbMole
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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