1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. Bisantrene

Bisantrene (Synonyms: CL216942)

Cat. No.: HY-100875 Purity: 95.44%
Handling Instructions

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

For research use only. We do not sell to patients.

Bisantrene Chemical Structure

Bisantrene Chemical Structure

CAS No. : 78186-34-2

Size Price Stock Quantity
10 mg USD 66 In-stock
Estimated Time of Arrival: December 31
25 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 240 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target[1]

Topoisomerase II

 

In Vivo

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 Ki 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 Ki, 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].

Clinical Trial
Molecular Weight

398.46

Formula

C₂₂H₂₂N₈

CAS No.

78186-34-2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : < 0.1 mg/mL (insoluble)

References
Kinase Assay
[1]

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].

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

References
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Bisantrene
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