An inhibitor of tubulin polymerization
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BNC-105 is an inhibitor of tubulin polymerization.1 It inhibits bovine tubulin polymerization in a cell-free assay (EC50 = 3 ?M). BNC-105 inhibits the proliferation of human umbilical vein endothelial cells (HUVECs) and human abdominal aorta endothelial cells (HAAECs; EC50s = 0.31 and 0.1 nM, respectively). It inhibits the proliferation of MCF-7 breast cancer cells (IC50 = 2.4 nM), as well as a panel of 9 additional cancer cell lines (IC50s = 0.16-18.4 nM).2 BNC-105 (1 nM) inhibits HUVEC capillary tube formation in a Matrigel? assay.1
1.Kremmidiotis, G., Leske, A.F., Lavranos, T.C., et al.BNC105: A novel tubulin polymerization inhibitor that selectively disrupts tumor vasculature and displays single-agent antitumor efficacyMol. Cancer Ther.9(6)1562-1573(2010) 2.Flynn, B.L., Gill, G.S., Grobelny, D.W., et al.Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting propertiesJ. Med. Chem.54(17)6014-6027(2011)
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