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Beschreibung

A cell-permeable ortho-hydroxybenzylamino compound that displays anti-tumor properties. Acts as a potent, selective, and irreversible inhibitor of CDC25 phosphatase family (IC50 = 2.4, 3.9, 6.3, 5.4, and 4.6 µ,M for 25A, 25B2, 25B3, 25C, and 25C-cat, respectively). Displays ~20-fold greater selectivity for CDC25 phosphatases compared to CD45 tyrosine phosphatase. Shown to delay cell cycle progression in vitro (IC50 in the range of 7.2-32.6 µ,M), and reduces tumor growth in athymic mice xenografted with the human pancreatic cell MIA PaCa-2 (15 mg/kg, i.p. route)., A cell-permeable ortho-hydroxybenzylamino compound that displays antitumor properties. Acts as a potent, selective and irreversible inhibitor of CDC25 phosphatase family (IC50 = 2.4, 3.9, 6.3, 5.4, and 4.6 µ,M for 25A, 25B2, 25B3, 25C, and 25C-cat, respectively). Displays ~20-fold greater selectivity for CDC25 phosphatases over CD45 tyrosine phosphatase. Shown to delay cell cycle progression in vitro (IC50 = ~7.2-32.6 µ,M), and reduces tumor growth in athymic mice xenografted with the human pancreatic cells MIA PaCa-2 (15 mg/kg, i.p. route).

Strukturformel

N-(2-Hydroxy-3-methoxy-5-dimethylamino)benzyl, N'-(2-(4-nitrophenethyl))

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