ATC code L01XX01 (WHO) Biological half-life 8-9 hours PubChem CID 2179 Molar mass 393.46 g/mol | Protein binding 96 to 98% CAS Number 51264-14-3 DrugBank DB00276 CAS ID 51264-14-3 | |
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Amsacrine meaning
Amsacrine (synonyms: m-AMSA, acridinyl anisidide) is an antineoplastic agent.
Contents
It has been used in acute lymphoblastic leukemia.
Medical vocabulary what does amsacrine mean
Mechanism
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). In contrast, the structurally similar o-AMSA differing in the position of the methoxy substituent group on the anilino-ring have little ability to poison topoisomerase II despite of its intercalative behavior, suggesting that intercalation of the molecule in itself is insufficient to trap topoisomerase II as a covalent complex on DNA.