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Overview
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Background
ENMD-2076 is an orally bioavailable, small molecule inhibitor of Aurora kinases with IC50 values of 14nM and 350nM, respectively against Aurora Kinase A and Aurora Kinase B [1].Besides Aurora kinases, ENMD-2076 inhibits multiple kinases involved in various cellular activities. Overexpression of Aurora Kinase A has been found in breast cancers and ENMD-2076 is thereby studied in breast cancers. It is reported that ENMD-2076 differentially inhibits 29 breast cancer cell lines with IC50 values ranged from 0.25 to 16.1μM. In the clonogenic assays, ENMD-2076 totally suppresses the colony formation in the sensitiveMDA-MB-468 cell line and decreases the formation in theHCC1806, SK-BR-3, and BT474 cell lines. ENMD-2076 is also reported to cause a G2 cell-cycle arrest at 1.25μM. Moreover, ENMD-2076 shows antitumor activity in TNBC xenograft models. Apart from the breast cancers, ENMD-2076 is developed in hematological malignancies therapy. The clinical trials have already conducted in Phase II [1, 2].
[1] Diamond JR, Eckhardt SG, Tan AC, Newton TP, Selby HM, Brunkow KL, Kachaeva MI, Varella-Garcia M, Pitts TM, Bray MR, Fletcher GC, Tentler JJ. Predictive biomarkers of sensitivity to the aurora and angiogenic kinase inhibitor ENMD-2076 in preclinical breast cancer models. Clin Cancer Res. 2013 Jan 1;19(1):291-303.
[2] How J, Yee K. ENMD-2076 for hematological malignancies. Expert Opin Investig Drugs. 2012 May;21(5):717-32.
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