A selective inhibitor of RNA polymerase I-driven transcription of rRNA (IC50s = 142

CX-5461 – 1 mg

Brand:
Cayman
CAS:
1138549-36-6
Storage:
-20
UN-No:
Non-Hazardous - /

CX-5461 is an inhibitor of ribosomal RNA (rRNA) synthesis. It selectively inhibits RNA polymerase I-driven transcription of rRNA in HCT116, A375, and MIA PaCa-2 tumor cells (IC50s = 142, 113, and 54 nM, respectively) without affecting RNA polymerase II (IC50 > 25µM), DNA replication, or protein translation.{30876,30877} At 50 mg/kg, CX-5461 demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.{30876}  

 

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Description

A selective inhibitor of RNA polymerase I-driven transcription of rRNA (IC50s = 142, 113, and 54 nM in HCT116, A375, and MIA PaCa-2 tumor cells, respectively); demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models

Formal name: 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

Synonyms: 

Molecular weight: 513.6

CAS: 1138549-36-6

Purity: ≥98%

Formulation: A crystalline solid

Application|Mass Spectrometry||Product Type|Biochemicals|Analytical Standards||Research Area|Cancer

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