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BI 2536

Cat. No. M1672

BI 2536 Structure
Size Price Availability Quantity
10mg USD 175 In stock
50mg USD 540 In stock
200mg USD 1080 In stock
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Quality Control
Biological Activity

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.

Protocol
Cell Experiment
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.
Concentrations 1~100nM
Incubation time 72 hr
Animal Experiment
Animal models Nude mice bearing established HCT 116 tumors xenograft model
Formulation unknown
Dosages 50mg/kg once or twice weekly
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 521.66
Formula C28H39N7O3
CAS Number 755038-02-9
Purity >99%
Solubility DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BI 2536 supplier, PLK, inhibitors

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