CYT997 is an orally available inhibitor of microtubule polymerization (IC50 = ~3 μM) that blocks cell cycling at the G2-M phase, which leads to cell death. It is cytotoxic to a range of cancer cell lines (IC50s = 9-101 nM) and demonstrates antivascular activity in tumors both in vitro and in vivo. CYT997 is being examined in clinical trials for efficacy against advanced solid tumors.