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TAS 103 is an inhibitor of DNA topoisomerase I and II (IC50s = 2 and 6.5 µM, respectively).1 It stabilizes topoisomerase I-DNA and topoisomerase II-DNA cleavable complexes in KB cells when used at a concentration of 3 µM. It is cytotoxic to P388 and KB cells (IC50s = 1.1 and 9.6 nM, respectively). TAS 103 (15, 26, and 45 mg/kg per day) reduces pulmonary metastasis in murine B16-BL6 melanoma and UV-2237M fibrosarcoma models of lung metastasis. It also reduces tumor growth in a variety of human cancer mouse xenograft models.
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1. Antitumor activity of a novel quinoline derivative, TAS-