SSE15206 is a microtubule polymerization inhibitor that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells.

Microtubule:197 nM (GI50)

细胞经SSE15206处理后出现异常有丝分裂，导致由于纺锤体形成不完全而引起的G2/M阶段阻滞，这是一种常与干扰微管动态的药物相关联的表型。SSE15206能够克服包括多药耐药的KB-V1和A2780-Pac-Res细胞系在内的不同癌症细胞线对化疗化合物的抵抗，这些细胞系过表达MDR-1，使其成为针对多药耐药的领先优化研究中的有希望的候选物。

Fluorescence intensity of tubulin (4?μM) in the presence of colchicine (20?μM) and SSE15206 at indicated concentrations was measured. DMSO was used as a solvent control while 50?μM nocodazole was used as a positive control for colchicine displacement. Samples were incubated for 60?min at 37℃before measurement of fluorescence (excitation at 355?nm and emission at 460?nm). KB-V1 and A2780-Pac-Res cells were incubated with 5?μM rhodamine, for 1?hour at 37℃in the presence or absence of inhibitors. Cells were then washed twice with PBS and incubated in the efflux medium (their respective growth media) in the presence of DMSO, 20?μM verapamil, and 10?μM SSE15206 for 3?hours. The percentage of rhodamine 123 positive cells was determined . Experiments were done in duplicates with 4–5 readings for each sample in each experiment.