| 货号 | 11694-50mg |
| 描述 | DNA topoisomerases relax DNA torsional strain created during replication, transcription, recombination, repair, and chromosome condensation. The relaxation of DNA supercoiling by topoisomerase I at single-strand breaks enables anticancer agents to reversibly trap the complex by intercalating between DNA base pairs at the cleavage site, thus inhibiting religa Camptothecin is a cytotoxic, quinoline alkaloid, discovered as the active principle of extracts from the Chinese tree C. acuminate, that inhibits the DNA enzyme topoisomerase I (Top1). It binds the Top1-DNA cleavage complex, inducing DNA-strand breaks.1,2 Camptothecin has strong anti-tumor activity against a wide range of experimental tumors and inhibits both DNA and RNA synthesis in mammalian cells.3 It displays cytotoxity in HT-29 cells with an IC50 value of 10 nM and induces DNA damage at concentrations as low as 51 nM in whole cells and 12 nM in isolated nuclei in in vitroassays.4 |
| 别名 | MAG-CPT;NSC 94600; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Hsiang, Y.H.,Hertzberg, R.,Hecht, S., et al. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I. The Journal of Biological Chemisty 260(27), 14873-14878 (1985). 2.Marchand, C.,Antony, S.,Kohn, K.W., et al. A novel norindeniosoquinoline structure reveals a common interfacial inhibitor paradigm for ternary trapping of the topoisomerase I-DNA covalent complex. Molecular Cancer Therapeutics 5(2), 287-295 (2006). 3.Dancey, J., and Eisenhauer, E.A. Current perspectives on camptothecins in cancer treatment. Br. J. Cancer 74(3), 327-338 (1996). 4.Rothenberg, M.L. Topoisomerase I inhibitors: Review and update. Annals of Oncology 8(9), 837-855 (1997). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 348.4 |
| 分子式 | C20H16N2O4 |
| CAS号 | 2114454 |
| 稳定性 | ≥ 2 years |
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