E7016

CAS 902128-92-1 MFCD002128921

化学结构图

902128-92-1
SMILES: O=c1[nH]nc2c3cc(CN4CCC(O)CC4)ccc3oc3cccc1c32

化学属性

Mol. Weight349.383
Appearance Solid powder
SolubilitySoluble in DMSO, not in water

别名和识别编码

Chemical NameE7016
FormulaC20H19N3O3
Synonym E7016; E-7016; E 7016; GPI21016; GPI 21016; GPI-21016.
IUPAC Name10-((4-Hydroxypiperidin-1-yl)methyl)chromeno[4,3,2-de]phthalazin-3(2H)-one
InChIKeyHAVFFEMDLROBGI-UHFFFAOYSA-N
InChIInChI=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 SMILESO=C1NN=C2C3=C1C=CC=C3OC4=C2C=C(CN5CCC(O)CC5)C=C4
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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.

安全信息

Storage condition Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

系列性分类

  1. Medical Research Areas
  2. DNA Damage
  3. PARP

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