Inhibitor of microtubule polymerization,antimitotic
CAS：141430-65-1
分子式：C18H17N3O4S
分子量：371.41
纯度：98%
存储：Store at -20°C

Background:

ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic agent [1][2].
Microtubules are major structure of cells. They play an important role in cellular movement, intracellular transport, cell shape, cellular polarity, and the segregation of chromosomes during mitosis[1].
ABT-751 binds to the colchicine site on ß-tubulin and inhibits polymerization of microtubules, which block the G2/M phase of the cell cycle and promote apoptosis [1]. In endothelial cells, ABT-751 caused significant loss of microtubules and endothelial cell retraction within 1 h in a does-dependent and reversible way [2].
In a rat subcutaneous tumor model, ABT-751 (30 mg/kg, intravenously) reduced tumor perfusion in a rapid, transient way. And tumor perfusion decreased by 57% after 1 h [3]. In Calu-6 xenograft model, ABT-751 dosed at 100 and 75 mg/kg/day showed significant antitumor activity. In combination with cisplatin, ABT-751 enhanced the growth delay in a dose-dependent way [1].
参考文献:
[1]. Jorgensen TJ, Tian H, Joseph IB, et al. Chemosensitization and radiosensitization of human lung and colon cancers by antimitotic agent, ABT-751, in athymic murine xenograft models of subcutaneous tumor growth. Cancer Chemother Pharmacol, 2007, 59(6): 725-732.
[2]. Luo Y, Hradil VP, Frost DJ, et al. ABT-751, a novel tubulin-binding agent, decreases tumor perfusion and disrupts tumor vasculature. Anticancer Drugs, 2009, 20(6): 483-492.