Bisantrene dihydrochloride is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene dihydrochloride targets eukaryotic type II topoisomerases. Bisantrene dihydrochloride is a substrate of MDR1.
性状
Solid
IC50 & Target[1][2]
Topoisomerase
体外研究(In Vitro)
Bisantrene dihydrochloride promots DNase I cleavage at oligopurine-oligopyrimidine tracts and slightly reduces the cleavage activity at alternating purine-pyrimidine sequences.Bisantrene dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride (25, 50 and 100 mg/kg; i.p.; once) pretreats with macrophages shows antitumor effect to mice with P815 tumor cells injection.
Bisantrene dihydrochloride (10-150 mg/kg; i.v.; once) dose-dependently induces leukopenia in Neo mice. B cells and macrophages are targets for bisantrene dihydrochloride toxicity. has not independently confirmed the accuracy of these methods.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 : 5 mg/mL (10.61 mM; Need ultrasonic)配制储备液