CEP-9722
CEP-9722 is a small-molecule prodrug of CEP-8983, a novel 4-methoxy-carbazole inhibitor of the nuclear enzymes poly(ADP-ribose) polymerase (PARP) 1 and 2, with potential antineoplastic activity. Upon administration and conversion from CEP-9722, CEP-8983 selectively binds to PARP 1 and 2, preventing repair of damaged DNA via base excision repair (BER). This agent enhances the accumulation of DNA strand breaks and promotes genomic instability and apoptosis. CEP-8983 may potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell chemo- and radioresistance.
1: Penning TD. Small-molecule PARP modulators--current status and future therapeutic potential. Curr Opin Drug Discov Devel. 2010 Sep;13(5):577-86. Review. PubMed PMID: 20812149.
| Chemical | |
|---|---|
| CAS Num | 916574-83-9 |
| Chemical Formula | C24H26N4O3 |
| Molecular Weight | 418.497 |
| IUPAC Chemical Name | 11-methoxy-2-((4-methylpiperazin-1-yl)methyl)-4,5,6,7-tetrahydro-1H-cyclopenta[a]pyrrolo[3,4-c]carbazole-1,3(2H)-dione |
| Exact Mass | 418.20049 |
| Elemental Analysis | C, 68.88; H, 6.26; N, 13.39; O, 11.47 |
| Synonym | CEP-9722; CEP 9722; CEP9722 |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C1N(CN2CCN(C)CC2)C(C3=C1C4=C(C5=C3CCC5)NC6=C4C(OC)=CC=C6)=O |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >5 years if stored properly |
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