| Description | E7449 (UNII-9X5A2QIA7C) is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ～50 and ～50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate. |
| In vitro | E7449 shows no obvious inhibiotry effects on PARP3 or PARPs 6-16. E7449 traps PARP1 onto damaged DNA, and affects DNA repair pathways beyond homologous recombination (HR). E7449 most potnetly suppresses cells deficient in components of the HR pathway (BRCA1 and 2, CtIP, Rad54). E7449 (10 μM) inhibits Wnt signaling in SW480 cells[1]. |
| In vivo | E7449在100 mg/kg剂量下对肿瘤生长有适度的抑制作用，并且在与替莫唑胺(TMZ)结合时，通过口服10、30和100 mg/kg剂量显著增强了在小鼠黑色素瘤B16-F10同种移植模型中的抑制效果[1]。 |
| Target activity | TNKS1:50 nM (IC50), PARP2:1 nM (IC50), PARP1:2 nM (IC50), TNKS2:50 nM (IC50) |
| Synonyms | Stenoparib, UNII-9X5A2QIA7C |
| molecular weight | 317.34 |
| Molecular formula | C18H15N5O |
| CAS | 1140964-99-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 6.4 mg/mL (20.17 mM), Sonication and heating are recommended. |
| References | 1. McGonigle S, Chen Z, Wu J, et al. E7449: A dual inhibitor of PARP1/2 and tankyrase1/2 inhibits growth of DNA repair deficient tumors and antagonizes Wnt signaling. Oncotarget. 2015;6(38):41307-41323. doi:10.18632/oncotarget.5846 |