S86503 |
Bisantrene |
源叶(MedMol) | 96% |
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- 产品描述: Bisantrene is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene targets eukaryotic type II topoisomerases. Bisantrene is a substrate of MDR1
- 靶点: Topoisomerase II;Topoisomerase
- 体外研究:
Bisantrene promots DNase I cleavage at oligopurine-oligopyrimidine tracts and slightly reduces the cleavage activity at alternating purine-pyrimidine sequences. Bisantrene is an inhibitor of [3H]uridine incorporation into RNA and [3H]thymidine incorporation into DNA
- 体内研究:
Bisantrene is an antitumor agent active against a number of experimental tumors, including P388 leukemia, L1210 leukemia, Lieberman plasma cell tumor, B16 melanoma, colon tumor 26, and Ridgway osteogenic sarcoma. Bisantrene is effective over a dose range of 1.56 to 150 mg/kg depending upon the frequency, route, and schedule of the treatment and the tumor model used. Bisantrene (25, 50 and 100 mg/kg; i.p.; once) pretreats with macrophages shows antitumor effect to mice with P815 tumor cells injection. Bisantrene (10-150 mg/kg; i.v.; once) dose-dependently induces leukopenia in Neo mice. B cells and macrophages are targets for bisantrene toxicity
- 参考文献:
1. Sissi C, et al. DNA-binding preferences of Bisantrene analogues: relevance to the sequence specificity of drug-mediated topoisomerase II poisoning. Mol Pharmacol. 1998 Dec;54(6):1036-45. 2. Yap HY, et al. Bisantrene, an active new drug in the treatment of metastatic breast cancer. Cancer Res. 1983 Mar;43(3):1402-4. 3. Wang BS, et al. Activation of tumor-cytostatic macrophages with the antitumor agent 9,10-anthracenedicarboxaldehyde bis[(4,5-dihydro-1H-imidazole-2-yl)hydrazone] dihydrochloride (bisantrene). Cancer Res. 1984 Jun;44(6):2363-7. 4. Aksentijevich I, et al. Retroviral transfer of the human MDR1 gene confers resistance to bisantrene-specific hematotoxicity. Clin Cancer Res. 1996 Jun;2(6):973-80.
- 溶解性: Soluble in DMSO、H2O
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.51 ml 12.548 ml 25.096 ml 5 mM 0.502 ml 2.51 ml 5.019 ml 10 mM 0.251 ml 1.255 ml 2.51 ml 50 mM 0.05 ml 0.251 ml 0.502 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)