Etoposide-d₃

Etoposide-d₃ is intended for use as an internal standard for the quantification of etoposide (Item No. 12092) by GC- or LC-MS. Etoposide is a plant alkaloid and an inhibitor of topoisomerase II (IC₅₀ = 60.3 μM).^1,2 It inhibits proliferation of a variety of adenocarcinoma cells (IC₅₀s = 0.005-12,200 µM) and human umbilical vein endothelial (HUVEC) cells (IC₅₀ = 0.249 µM).³ It reduces tumor growth in an Ma human embryonal carcinoma mouse xenograft model when administered at a dose of 25 mg/kg, an effect that is enhanced by concomitant administration of the immunosuppressant cyclosporin A (Item No. 12088).⁴ Etoposide also inhibits nuclear receptor coactivator 3 (IC₅₀ = 2.48 µM).⁵ Formulations containing etoposide have been used in combination therapy in the treatment of cancer.

WARNING This product is not for human or veterinary use.

1. Chen, G.L., Yang, L., Rowe, T.C., et al. Nonintercalative antitumor drugs interfere with the breakage-reunion reaction of mammalian DNA topoisomerase II. The Journal of Biological Chemisty 259(21), 13560-13566 (1984).

2. Wu, W.B., Ou, J.B., Huang, Z.H., et al. Synthesis and evaluation of mansonone F derivatives as topoisomerase inhibitors. Eur. J. Med. Chem. 46(8), 3339-3347 (2011).

3. Drevs, J., Fakler, J., Eisele, S., et al. Antiangiogenic potency of various chemotherapeutic drugs for metronomic chemotherapy. Anticancer Res. 24, 1759-1764 (2004).

4. Osieka, R., Seeber, S., Pannenbäcker, R., et al. Enhancement of etoposide-induced cytotoxicity by cyclosporin A. Cancer Chemother. Pharmacol. 18(3), 198-202 (1986).

5. O'Malley, B. Luminescence-based cell-based high throughput dose response assay for inhibitors of the Steroid Receptor Coactivator 3 (SRC;NCOA3) - BioAssay summary.