WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205882
Description: E7449, also known as 2X-121, is an orally available small molecule inhibitor of the nuclear enzymes poly (ADP-ribose) polymerase (PARP) 1 and 2, with potential antineoplastic activity. Upon administration, E7449 selectively binds to PARP 1 and 2, thereby preventing the repair of damaged DNA via the base excision repair (BER) pathway. This agent enhances the accumulation of single and double strand DNA breaks and promotes genomic instability eventually leading to apoptosis. PARP 1/2 inhibitor E7449 may enhance the cytotoxicity of DNA-damaging agents and of radiotherapy. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA.
MedKoo Cat#: 205882
Chemical Formula: C18H15N5O
Exact Mass: 317.12766
Molecular Weight: 317.34
Elemental Analysis: C, 68.13; H, 4.76; N, 22.07; O, 5.04
Synonym: E7449; E 7449; E-7449; 2X-121; 2X 121; 2X121;
IUPAC/Chemical Name: 8-(isoindolin-2-ylmethyl)-2H-pyridazino[3,4,5-de]quinazolin-3(9H)-one
InChi Key: JLFSBHQQXIAQEC-UHFFFAOYSA-N
InChi Code: InChI=1S/C18H15N5O/c24-18-13-6-3-7-14-16(13)17(21-22-18)20-15(19-14)10-23-8-11-4-1-2-5-12(11)9-23/h1-7H,8-10H2,(H,22,24)(H,19,20,21)
SMILES Code: O=C1NN=C(N2)C3=C(C=CC=C31)N=C2CN(C4)CC5=C4C=CC=C5
1: Laurance J. Neurologists appeal to health secretary over withdrawal of drug for MS patients. BMJ. 2012 Nov 2;345:e7449. doi: 10.1136/bmj.e7449. PubMed PMID: 23125160.
2: Gilmore S, Hofmann-Wellenhof R, Muir J, Soyer HP. Lacunarity analysis: a promising method for the automated assessment of melanocytic naevi and melanoma. PLoS One. 2009 Oct 13;4(10):e7449. doi: 10.1371/journal.pone.0007449. PubMed PMID: 19823688; PubMed Central PMCID: PMC2758593.