1215208-65-3

MPT0B214 is a novel and potent microtubule inhibitor with potential anticancer activity. MPT0B214 inhibited tubulin polymerization through strongly binding to the tubulin's colchicine-binding site and had cytotoxic activity in a variety of human tumor cell lines. After treatment with MPT0B214, KB cells were arrested in the G2-M phase before cell death occurred, which were associated with upregulation of cyclin B1, dephosphorylation of Cdc2, phosphorylation of Cdc25C and elevated expression of the mitotic marker MPM-2. Furthermore, the compound induced apoptotic cell death through mitochondria/caspase 9-dependent pathway. Notably, several KB-derived multidrug-resistant cancer cell lines were also sensitive to MPT0B214 treatment. ( PLoS One. 2013;8(3):e58953).

MPT0B214 是一种微管抑制剂，通过与微管蛋白的秋水仙碱结合位点强烈结合来抑制微管蛋白聚合。MPT0B214 通过线粒体/caspase 9 依赖性途径诱导细胞凋亡 (apoptosis)，在多种人肿瘤细胞系中具有细胞毒性。MPT0B214 可用于肿瘤的研究。