10-((4-Hydroxypiperidin-1-yl)methyl)chromeno[4,3,2-de]phthalazin-3(2H)-one 10-((4-羟基哌啶-1-基)甲基)苯并吡喃并[4,3,2-de]酞嗪-3(2H)-酮
CAS 902128-92-1 MFCD002128921
化学结构图
SMILES: O=c1[nH]nc2c3cc(CN4CCC(O)CC4)ccc3oc3cccc1c32
化学属性
| Mol. Weight | 349.383 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | 10-((4-Hydroxypiperidin-1-yl)methyl)chromeno[4,3,2-de]phthalazin-3(2H)-one |
|---|---|
| Formula | C20H19N3O3 |
| Synonym | E7016; E-7016; E 7016; GPI21016; GPI 21016; GPI-21016. |
| IUPAC Name | 10-((4-Hydroxypiperidin-1-yl)methyl)chromeno[4,3,2-de]phthalazin-3(2H)-one |
| InChIKey | HAVFFEMDLROBGI-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H19N3O3/c24-13-6-8-23(9-7-13)11-12-4-5-16-15(10-12)19-18-14(20(25)22-21-19)2-1-3-17(18)26-16/h1-5,10,13,24H,6-9,11H2,(H,22,25) |
| Canonical SMILES | O=C1NN=C2C3=C1C=CC=C3OC4=C2C=C(CN5CCC(O)CC5)C=C4 |
| Chemical Name Translation | 10-((4-羟基哌啶-1-基)甲基)苯并吡喃并[4,3,2-de]酞嗪-3(2H)-酮 |
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产品应用
- 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.
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