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CU-201 is a network-targeted molecule that is designed to simultaneously inhibit HDAC, Abl and Src family kinases, the combination of which Curis scientists believe have synergistic interaction against cancer cells. Src family kinases are critical components of multiple signaling pathways that regulate cancer cell proliferation, survival, angiogenesis and metastasis. Thus, as a network disrupting agent that directly targets multiple nodes of genetic and epigenetic dysregulation, CU-201 is expected to impact processes as diverse as proliferation, survival, metastasis and angiogenesis in cancer. In vitro studies demonstrate that CU-201 is able to potently inhibit class I and class II HDACs, Src and Bcr-Abl. It has been shown to outperform single target agents in proliferation assays of hematologic and solid tumor lines and to inhibit migration and invasion of cancer cell lines in vitro. In vivo, it displays potent anti-tumor activity in a variety of hematologic and solid tumor models, including subcutaneous, metastatic and orthotopic models.


 

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