Vosaroxin

Vosaroxin is an inhibitor of topoisomerase II.¹ It induces relaxation of supercoiled DNA with an IC₅₀ value of 3.2 µg/ml in a cell-free assay. It induces DNA double-strand breaks in CCRF-CEM cells and cell cycle arrest at the G₂ phase in A549 cells in a concentration-dependent manner.² Vosaroxin inhibits proliferation in a panel of 15 cancer cell lines, including cancer cells resistant to doxorubicin (Item No. 15007), etoposide (Item No. 12092), or cisplatin (Item No. 13119), with IC₅₀ values ranging from 0.04 to 1.15 µM.³ It inhibits tumor growth in multidrug-resistant SBC-3/ETP or PC-14/CDDP mouse xenograft models when administered at a dose of 20 mg/kg.

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1. Tsuzuki, Y., Tomita, K., Shibamori, K.-i., et al. Synthesis and structure-activity relationships of novel 7-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acids as antitumor agents. Part 2. J. Med. Chem. 47(8), 2097-2109 (2004).

2. Hawtin, R.E., Stockett, D.E., Byl, J.A.W., et al. Voreloxin is an anticancer quinolone derivative that intercalates DNA and poisons topoisomerase II. PLoS One 5(4), e10186 (2010).

3. Hoch, U., Lynch, J., Sato, Y., et al. Voreloxin, formerly SNS-595, has potent activity against a broad panel of cancer cell lines and in vivo tumor models. Cancer Chemother. Pharmacol. 64(1), 53-65 (2009).