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| 化学名: | | | 英語化学名: | MPT0B214 | | 别名: | MPT0B214;Methanone, (5-amino-6-methoxy-2-quinolinyl)(3,4,5-trimethoxyphenyl)- | | CAS番号: | 1215208-65-3 | | 分子式: | C20H20N2O5 | | 分子量: | 368.38 | | EINECS: | | | カテゴリ情報: | | | Mol File: | 1215208-65-3.mol |  |
| 融点 | 184.3-185.2 °C(Solv: methanol (67-56-1)) | | 沸点 | 580.5±50.0 °C(Predicted) | | 比重(密度) | 1.256±0.06 g/cm3(Predicted) | | 酸解離定数(Pka) | 1.02±0.10(Predicted) |
| | MPT0B214 Usage And Synthesis |
| 説明 | 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). | | 使用 | MPT0B214 is a microtubule inhibitor that strongly binds to the colchicine binding site of tubulin, preventing tubulin polymerization. MPT0B214 induces apoptosis through a mitochondrial/caspase 9 dependent pathway and shows cytotoxicity across various human tumor cell lines. MPT0B214 can be used for cancer research[1]. | | 参考文献 | [1] Chiang NJ, et al. A novel synthetic microtubule inhibitor, MPT0B214 exhibits antitumor activity in human tumor cells through mitochondria-dependent intrinsic pathway. PLoS One. 2013;8(3):e58953. DOI:10.1371/journal.pone.0058953 |
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