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Beschreibung

A cell permeable benzenesulfonamide Carbonic Anhydrase (CA) inhibitor that is selective for human hCA IX and hCA XII (Ki = 0.9 nM and 5.7 nM, respectively) against two other physiologically relevant hCA isoforms (Ki = 23.4 nM and 15 nM for hCA I and hCA II, respectively), as compared with another CA inhibitor AAZ (Ki = 250 nM, 12 nM, 25 nM, and 5.7 nM for hCA I, hCA II, hCA IX, and hCA XII, respectively). It is shown to effectively inhibit the formation of metastases by 4T1 breast cancer cells in a mouse model dose-dependently at pharmacologic concentrations of 15-45 mg/kg.