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Belinostat is an inhibitor of class I histone deacetylases (HDACs; IC50s = 0.041, 0.125, 0.03, and 0.216 µM for HDAC1, -2, -3, and -8, respectively) and class II HDACs (IC50s = 0.115, 0.082, 0.067, and 0.128 µM for HDAC4, -6, -7, and -9, respectively).1 It inhibits HDAC activity in HeLa cell lysates (IC50 = 0.027 µM) and the proliferation of A2780 ovarian, HCT116 colon, Calu-3 lung, and Hs 852.T melanoma cells (IC50s = 0.2, 0.2, 0.66, and 3.37 µM, respectively).2 It reduces tumor growth in an A2780 mouse xenograft model when administered at doses of 10, 20, and 40 mg/kg. Formulations containing belinostat have been used in the treatment of relapsed or refractory peripheral T cell lymphoma.
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1. Determination of the class and isoform selectivity of small-
2. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101. Mol. Cancer Ther. 2(8), 721-728 (2003).