CX-5461

Term ID

CHEBI:156287

Synonyms

• 2-(4-methyl-1,4-diazepan-1-yl)-N-[(5-methylpyrazin-2-yl)methyl]-5-oxo-5H-[1,3]benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide
• 2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-N-[(5-methyl-2-pyrazinyl)methyl]-5-oxo-5H-benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide
• CX 5461
• CX5461

Definition

An organic heterotetracyclic compound that is 5-oxo-5H-[1,3]benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxylic acid substituted by a 4-methyl-1,4-diazepan-1-yl group at position 2 and in which the carboxy group at position 6 is substituted by a [(5-methylpyrazin-2-yl)methyl]nitrilo group. An inhibitor of ribosomal RNA (rRNA) synthesis which specifically inhibits RNA polymerase I-driven transcription of rRNA in several cancer cell lines. It is currently in phase I/II clinical trials for advanced hematologic malignancies and triple-negative breast cancer with BRCA1/2 mutation.

References

• cas:1138549-36-6
• lincs.smallmolecule:LSM-6342
• pubmed:21159662
• pubmed:30016731
• pubmed:30542116
• pubmed:30879743
• pubmed:31092402
• pubmed:31183313
• pubmed:31210846
• pubmed:31341008
• pubmed:31557908
• pubmed:31817270
• pubmed:32041867
• pubmed:32414869
• pubmed:32457376
• pubmed:32719798

Ontology

ChEBI  ( EBI )