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ENMD-2076 is a novel, orally bioavailable multitargeted antiangiogenic and Aurora kinase inhibitor with IC50 of 3, 13, 350, 23, 40, 93 and 120 nM for Flt-3, AurA, AurB, Src, KDR/VEGFR2 and FGFR1. ENMD-2076 is relatively selective for the Aurora A isoform in comparison to Aurora B. ^[1] ENMD-2076 has demonstrated significant, dose-dependent preclinical activity as a single agent, including tumor regression, in multiple xenograft models (e.g. breast, colon, leukemia), as well as activity towards ex vivo-treated human leukemia patient cells. ENMD-2076 is currently in Phase 1 clinical studies in solid tumors and multiple myeloma. ENMD-2076 demonstrated robust antitumor activity against cell line and patient-derived xenograft models of CRC that is detectable by functional imaging, supporting clinical investigation of this agent in human colorectal cancer. ^[1][2]

• Assessment of the In vivo Antitumor Effects of ENMD-2076, a Novel Multitargeted Kinase Inhibitor, against Primary and Cell Line-Derived Human Colorectal Cancer Xenograft Models Erica L. Bradshaw-Pierce, Natalie J. Serkova, et al. Clin Cancer Res 2010;16:2989-2998
• ENMD-2076 Is an Orally Active Kinase Inhibitor with Antiangiogenic and Antiproliferative Mechanisms of Action Richard D. Brokx, Trisha A. Denny, et al. Mol Cancer Ther 2011;10:126-137

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