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BI 2536

Cat. No. M1672
BI 2536 Structure
Synonym:

BI 2536

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 110  USD110 In stock
2mg USD 49  USD49 In stock
5mg USD 85  USD85 In stock
25mg USD 150  USD150 In stock
50mg USD 250  USD250 In stock
100mg USD 450  USD450 In stock
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Quality Control & Documentation
Biological Activity

BI 2536 is a novel, highly selective, potent dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively. BI 2536 causes HeLa cells to accumulate with a 4N DNA content, indicative of a cell-cycle block in either G2 phase or mitosis. In addition to HeLa cells, BI 2536 potently inhibits the proliferation of a panel of 32 human cancer cell lines, representing diverse organ derivations (including carcinomas of the breast, colon, lung, pancreas, and prostate, melanomas, and hematopoietic cancers) and varied patterns of tumor suppressor or oncogene mutations (including RB1, TP53, PTEN, andKRAS status).

In vivo, BI 2536 (40-50 mg/kg, i.v.) blocks the growth of human cancer xenografts in immunodeficient, nu/nu mice. Consecutive cycles of 40-50 mg/kg BI 2536 given i.v. once or twice per week are 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 (treated versus the control (T/C) value 0.3%) and a T/C value of 16% with once per week treatment.

Product Citations
Customer Product Validations & Biological Datas
Source Oncogene (2018). Figure 2. Bi 2536 (AbMole BioScience)
Method The kinase activity assay
Cell Lines HeLa cells
Concentrations 1 μM
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.
Protocol (for reference only)
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.
Chemical Information
Molecular Weight 521.66
Formula C28H39N7O3
CAS Number 755038-02-9
Solubility (25°C) DMSO 50 mg/mL
Storage 2-8°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Haupenthal et al. Neoplasia. Reduced efficacy of the Plk1 inhibitor BI 2536 on the progression of hepatocellular carcinoma due to low intratumoral drug levels.

[2] Mross et al. Br J Cancer. 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.

[3] Ellis et al. Clin Lung Cancer. 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.

[4] de Oliveira et al. J Drugs Dermatol. In vitro PLK1 inhibition by BI 2536 decreases proliferation and induces cell-cycle arrest in melanoma cells.

[5] Frost et al. Curr Oncol. Phase i study of the Plk1 inhibitor BI 2536 administered intravenously on three consecutive days in advanced solid tumours.

[6] Pezuk et al. Clin Exp Med. Antiproliferative in vitro effects of BI 2536-mediated PLK1 inhibition on cervical adenocarcinoma cells.

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