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Bisantrene dihydrochloride

(Synonyms: CL-216942 dihydrochloride) 目录号 : GC68772

Bisantrene 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。

Bisantrene dihydrochloride Chemical Structure

Cas No.:71439-68-4

规格 价格 库存 购买数量
10mg
¥495.00
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25mg
¥1,080.00
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50mg
¥1,800.00
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100mg
¥2,880.00
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Sample solution is provided at 25 µL, 10mM.

Description

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.

化学性质

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
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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
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