E7016
E7016, also known as GPI21016, is an inhibitor of the nuclear enzyme poly (ADP-ribose) polymerase (PARP) with potential chemo- and/or radiosensitizing activity. PARP inhibitor E7016 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks and promotes genomic instability and eventually leads to apoptosis. In addition, this agent may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA and is activated by single-strand DNA breaks.
1: Lai WG, Farah N, Moniz GA, Wong YN. A Baeyer-Villiger oxidation specifically catalyzed by human flavin-containing monooxygenase 5. Drug Metab Dispos. 2011 Jan;39(1):61-70. Epub 2010 Oct 14. PubMed PMID: 20947616.
2: Crispi S, Calogero RA, Santini M, Mellone P, Vincenzi B, Citro G, Vicidomini G, Fasano S, Meccariello R, Cobellis G, Menegozzo S, Pierantoni R, Facciolo F, Baldi A, Menegozzo M. Global gene expression profiling of human pleural mesotheliomas: identification of matrix metalloproteinase 14 (MMP-14) as potential tumour target. PLoS One. 2009 Sep 15;4(9):e7016. PubMed PMID: 19753302; PubMed Central PMCID: PMC2737627.
3: Russo AL, Kwon HC, Burgan WE, Carter D, Beam K, Weizheng X, Zhang J, Slusher BS, Chakravarti A, Tofilon PJ, Camphausen K. In vitro and in vivo radiosensitization of glioblastoma cells by the poly (ADP-ribose) polymerase inhibitor E7016. Clin Cancer Res. 2009 Jan 15;15(2):607-12. PubMed PMID: 19147766.
2: Crispi S, Calogero RA, Santini M, Mellone P, Vincenzi B, Citro G, Vicidomini G, Fasano S, Meccariello R, Cobellis G, Menegozzo S, Pierantoni R, Facciolo F, Baldi A, Menegozzo M. Global gene expression profiling of human pleural mesotheliomas: identification of matrix metalloproteinase 14 (MMP-14) as potential tumour target. PLoS One. 2009 Sep 15;4(9):e7016. PubMed PMID: 19753302; PubMed Central PMCID: PMC2737627.
3: Russo AL, Kwon HC, Burgan WE, Carter D, Beam K, Weizheng X, Zhang J, Slusher BS, Chakravarti A, Tofilon PJ, Camphausen K. In vitro and in vivo radiosensitization of glioblastoma cells by the poly (ADP-ribose) polymerase inhibitor E7016. Clin Cancer Res. 2009 Jan 15;15(2):607-12. PubMed PMID: 19147766.
| Chemical | |
|---|---|
| CAS Num | 902128-92-1 |
| Chemical Formula | C20H19N3O3 |
| Molecular Weight | 349.383 |
| IUPAC Chemical Name | 10-((4-Hydroxypiperidin-1-yl)methyl)chromeno[4,3,2-de]phthalazin-3(2H)-one |
| Exact Mass | 349.14264 |
| Elemental Analysis | C, 68.75; H, 5.48; N, 12.03; O, 13.74 |
| Synonym | E7016; E-7016; E 7016; GPI21016; GPI 21016; GPI-21016. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C1NN=C2C3=C1C=CC=C3OC4=C2C=C(CN5CCC(O)CC5)C=C4 |
| Biological | |
| Targets and Effects | PARP inhibitor |
| 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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