Bisantrene  (Synonyms: CL216942)

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^[1][2][3][4].

Bisantrene promots DNase I cleavage at oligopurine-oligopyrimidine tracts and slightly reduces the cleavage activity at alternating purine-pyrimidine sequences^[1].
Bisantrene is an inhibitor of [³H]uridine incorporation into RNA and [³H]thymidine incorporation into DNA^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[3].
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^[3].
Bisantrene (25, 50 and 100 mg/kg; i.p.; once) pretreats with macrophages shows antitumor effect to mice with P815 tumor cells injection^[3].
Bisantrene (10-150 mg/kg; i.v.; once) dose-dependently induces leukopenia in Neo mice. B cells and macrophages are targets for bisantrene toxicity^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

398.46

C₂₂H₂₂N₈

78186-34-2

Solid

Orange to red

C12=CC=CC=C1C(/C=N/NC3=NCCN3)=C4C(C=CC=C4)=C2/C=N/NC5=NCCN5

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]