Bisantrene dihydrochloride
(Synonyms: CL-216942 dihydrochloride) 目录号 : GC68772Bisantrene dihydrochloride 是高效的抗癌剂,它通过影响 DNA 插入发挥细胞毒性。Bisantrene dihydrochloride 靶向真核生物的拓扑异构酶 II。Bisantrene dihydrochloride 是MDR1 的底物。
Cas No.:71439-68-4
Sample solution is provided at 25 µL, 10mM.
Bisantrene didrochloride is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene didrochloride targets eukaryotic type II topoisomerases. Bisantrene didrochloride is a substrate of MDR1[1][2][3][4].
Bisantrene didrochloride promots DNase I cleavage at oligopurine-oligopyrimidine tracts and slightly reduces the cleavage activity at alternating purine-pyrimidine sequences[1].
Bisantrene didrochloride is an inhibitor of [3H]uridine incorporation into RNA and [3H]tmidine incorporation into DNA[2].
Bisantrene didrochloride 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[3].
Bisantrene didrochloride 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[3].
Bisantrene didrochloride (25, 50 and 100 mg/kg; i.p.; once) pretreats with macrophages shows antitumor effect to mice with P815 tumor cells injection[3].
Bisantrene didrochloride (10-150 mg/kg; i.v.; once) dose-dependently induces leukopenia in Neo mice. B cells and macrophages are targets for bisantrene didrochloride toxicity[4].
[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 , 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-anthracenedicarboxaldede bis[(4,5-didro-1H-imidazole-2-yl)drazone] didrochloride (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.
Cas No. | 71439-68-4 | SDF | Download SDF |
别名 | CL-216942 dihydrochloride | ||
分子式 | C22H24Cl2N8 | 分子量 | 471.39 |
溶解度 | DMSO : 5 mg/mL (10.61 mM; Need ultrasonic) | 储存条件 | 4°C, away from moisture |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.1214 mL | 10.6069 mL | 21.2139 mL |
5 mM | 0.4243 mL | 2.1214 mL | 4.2428 mL |
10 mM | 0.2121 mL | 1.0607 mL | 2.1214 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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