Amsacrine

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Amsacrine
Systematic (IUPAC) name
N-(4-(acridin-9-ylamino)-3-methoxyphenyl)methanesulfonamide
Identifiers
CAS number 51264-14-3
ATC code L01XX01
PubChem 2179
DrugBank APRD00064
Chemical data
Formula C21H19N3O3S 
Mol. mass 393.46 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 96 to 98%
Metabolism  ?
Half life 8-9 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes  ?

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Amsacrine

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Overview

Amsacrine is an antineoplastic agent. Its planar fused ring system can intercalate into the DNA of tumor cells, thereby altering the major and minor groove proportions. These alterations to DNA structure inhibit both DNA replication and transcription by reducing association between the affected DNA and: DNA polymerase, RNA polymerase and transcription factors.

Amsacrine also expresses topoisomerase inhibitor activity, specifically inhibiting topoisomerase II (compares with the better known agent etoposide).[1]

References

  1. Genetic Response to Metals. Sarkar, Bibudhendra. CRC Press, 1995. ISBN 9780824796150



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