Bisantrene 是高效的抗癌剂,它通过影响 DNA 插入发挥细胞毒性。Bisantrene 靶向真核生物的拓扑异构酶 II。Bisantrene 是 MDR1 的底物。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
Topoisomerase II
体外研究(In Vitro)
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 [H]uridine incorporation into RNA and [H]thymidine incorporation into DNA. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : 1 mg/mL (2.51 mM; ultrasonic and warming and heat to 80°C)H2O : 0.1 mg/mL (0.25 mM; ultrasonic and warming and heat to 50°C)