Bisantrene is a highly effective antitumor drug, targets eukaryotic type II topoisomerases.

Bisantrene shows an outstanding ability to form a complex with DNA. Bisantrene exhibits the most effective binding (even neglecting electrostatic contacts), followed by the 9-substituted compounds and finally by 1-IHA. Bisantrene congeners retained a remarkable capacity for binding to the single-stranded structure. In comparison with the K_i values found for double-stranded DNA, 9-IHA shows a 2-fold increase, 1-IHA maintains the same values, and aza-9-IHA exhibits a modest reduction. On the other hand, Bisantrene, although undergoing a 6-fold reduction in K_i, still exhibits an affinity constant of the order of 10⁶ M^-1. Bisantrene promots DNase I cleavage at oligopurine-oligopyrimidine tracts; conversely, it slightly reduces the cleavage activity at alternating purine-pyrimidine sequences^[1]. Bisantrene is an active new drug in the treatment of metastatic breast cancer. Bisantrene is an inhibitor of [³H]uridine incorporation into RNA and [³H]thymidine incorporation into DNA^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

398.46

C₂₂H₂₂N₈

78186-34-2

比生群；必桑郡

Room temperature in continental US; may vary elsewhere.

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)

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储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-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。

• [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.

Measurements are carried out at 25°C in ETN buffer (1 mM EDTA, 10 mM Tris, pH 7.0, with NaCl to obtain the desired ionic strength). Binding is monitored spectrophotometrically or fluorometrically, in the ligand absorption or emission region, respectively, after addition of scalar amounts of DNA to a freshly prepared drug solution. To avoid large systematic inaccuracies resulting from experimental errors in extinction coefficients or fluorescence quantum yield, the range of bound drug fractions is 0.15-0.85. Data are evaluated. Spectroscopic measurements are made with a Perkin-Elmer Lambda 5 apparatus and a MPF66 fluorometer, both equipped with a Haake F3-C thermostat^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.