Uses
ENMD-2076 (ENMD-981693, ENMD2076) is a 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.
Biological Activity
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
References
[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.
