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Biological Activity:
Highly potent and oral inhibitor of histone deacetylase (HDAC) with IC5o of HDAC1 to be 0.23 nM; an investigational drug against human pancreatic cancer, T cell lymphoma and other types of malignant diseases.
In vitro LBH 589 induces cell cycle arrest and apoptosis through both caspase dependent and caspase independent pathways in various tumor cell types at nanomolar concentrations. In vivo LBH 589 inhibits tumor angiogenesis as evidenced by blocking new blood vessel formation in human prostate carcinoma cell PC 3 xenografts.
References: online
P Maiso et al. The Histone Deacetylase Inhibitor LBH589 Is a Potent Antimyeloma Agent that Overcomes Drug Resistance. Cancer Res. 2006, 66(11), 5781-5789. [online]
AA Lane and BA Chabner. Histone Deacetylase Inhibitors in Cancer Therapy. J. Clin. Oncol. 2009, 27(32), 5459 - 5468. [online]
L Ellis et al. The histone deacetylase inhibitors LAQ824 and LBH589 do not require death receptor signaling or a functional apoptosome to mediate tumor cell death or therapeutic efficacy. Blood, 2009, 114(2), 380 - 393.
Chemical Name: (E)-N-hydroxy-3-[4-[[2-(2-methyl-1H-indol-3-yl)ethylamino]methyl]phenyl]prop-2-enamide
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