| 应用 |
A potent inhibitor of PARP |
| 产品介绍 |
Olaparib (AZD2281, Ku-0059436)是一种选择性的PARP1/2抑制剂，IC50为5 nM/1 nM，比对Tankyrase-1的作用强300倍。 |
| 备注 |
Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM, 300-times less effective against tankyrase-1. Phase 1/2. |
| 生化机理 |
Olaparib is a potent inhibitor of both PARP-1 and PARP-2, with IC50 = 5 nM and 1 nM, respectively. Olaparib is strongly sensitive to KB2P cells due to suppression of base excision repair by PARP inhibition, which may result in the conversion of single-strand breaks to double-strand breaks during DNA replication, thus activating BRCA2-dependent recombination pathways |
| 别名 |
KU-0059436;奥拉帕尼; 1-(环丙甲酰基)-4-[5-[(3,4-二氢-4-氧代-1-酞嗪基)甲基]-2-氟苯甲酰]哌嗪;AZD2281;KU-0059436;KU0059436;AZD-2281;KU0059436;AZD 2281;1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine |
