| Description | Venadaparib (NOV140101) (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib is insensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSBs) and can be used in solid tumor research. |
| In vitro | Venadaparib significantly inhibits PARP1-mediated PAR expression with an EC50?of 0.5 nM In DNA damage-induced Hela cells[1]. |
| In vivo | Oral administration of Venadaparib significantly inhibits PAR(>90%) in tumor tissues until 24 hr post-dose in the germline BRCA1-mutated ovarian cancer PDX model. Venadaparib also dose-dependently inhibits potent tumor growth compared to the Olaparib treatment group[1]. |
| Target activity | PARP1/PARP2:1.4 nM/1.0 nM, PARP1:0.5 nM(EC50) |
| Synonyms | NOV140101, IDX-1197 |
| molecular weight | 406.45 |
| Molecular formula | C23H23FN4O2 |
| CAS | 1681017-83-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 90 mg/mL (221.43 mM) |
| References | 1. Cheng-Chang Chen, et al. A Small Molecule Restores Function to TRPML1 Mutant Isoforms Responsible for Mucolipidosis Type IV. Nat Commun. 2014 Aug 14;5:4681. |