Bisantrene|cas 78186-34-2|DC Chemicals

Cas No.:	78186-34-2
Chemical Name:	CL216942;CL-216942;CL 216942
Synonyms:	CL216942;CL-216942;CL 216942
SMILES:	C12=CC=CC=C1C(/C=N/NC3=NCCN3)=C4C(C=CC=C4)=C2/C=N/NC5=NCCN5
Formula:	C₂₂H₂₂N₈
M.Wt:	398.46
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[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 trea

Description:

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

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].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

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