CX5461
- Catalog NO.:A894301
- CAS No. : 1138549-36-6
- Molecular Formula:C27H27N7O2S
- Molecular Weight: 513.61
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Product Details
CAS Number | 1138549-36-6 | Appearance | |
Catalog Number | A894301 | MDL Number | MFCD21609261 |
Molecular Formula | C27H27N7O2S | Molecular Weight | 513.61 |
Boiling Point | Melting Point | ||
Flash Point | Density | ||
Synonyms | 2-(4-methyl-1,4-diazepan-1-yl)-N-((5-methylpyrazin-2-yl)methyl)-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxamide;CX-5461 | ||
Storage Condition | Store in a tightly closed container,in a cool and dry place |
Safety
GHS Pictogram | |||
Signal Word | Warning | UN Number | |
Hazard Statements | H302-H315-H319-H335 | Class | |
Precautionary Statements | P261-P305+P351+P338 | Packing Group |
Description
CX-5461 is a first-in-class non-genotoxic small molecule targeted inhibitor of RNA polymerase I (Pol I) that activates the p53 pathway without causing DNA damage. CX-5461 selectively inhibits rRNA synthesis by Pol I in the nucleolus, but does not inhibit mRNA synthesis by RNA Polymerase II (Pol II) and does not inhibit DNA replication or protein synthesis. Inhibition of Pol I results in nucleolar stress and release of ribosomal proteins (RP) from the nucleolus. The RP bind to Mdm2 and liberate p53 to orchestrate apoptosis in cancer cells. CX-5461 demonstrates a favorable preclinical profile, potently and selectively kills cancer cells, demonstrates robust in vivo efficacy in multiple models, and has demonstrated oral bioavailability in multiple species. |