Description
General description
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 µM 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 µM), and reduces tumor growth in athymic mice xenografted with the human pancreatic cell MIA PaCa-2 (15 mg/kg, i.p. route).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CDC25A
Product does not compete with ATP.
Reversible: no
Target IC₅₀: 2.4, 3.9, 6.3, 5.4, and 4.6 µM for CDC25 phosphatase family 25A, 25B2, 25B3, 25C, and 25C-cat, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Unstable in aqueous solution.
Other Notes
Brezak, M.C., et al. 2004. Cancer Res.64, 3320.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
