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CUDC-907 is a dual inhibitor of HDACs and phosphatidylinositol 3-kinases (PI3Ks).1 It inhibits HDAC activity in HeLa nuclear extracts (IC50 = <0.1 μM) as well as the PI3K isoforms PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50s = <0.1, <1, <1, and <0.1 μM, respectively, for human recombinant enzymes). CUDC-907 inhibits cell growth in a panel of colon, pancreatic, non-small cell lung cancer (NSCLC), and multiple myeloma cells (IC50s = <10-100 nM). It induces cell cycle arrest at the G2/M phase and apoptosis and decreases cellular migration and invasion in FTC-133, THJ-29T, XTC-1, and 8505C thyroid cancer cell lines in a concentration-dependent manner.2 CUDC-907 (75 mg/kg) reduces tumor growth, the number of liver metastases, and HDAC2 expression in tumor tissue in the FTC-133 mouse xenograft model.
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1. Treatment of cancers having k-
2. Dual Inhibition of HDAC and tyrosine kinase signaling pathways with CUDC-