[S(R)]-N-[(1R)-1-[2-(二苯基膦)苯基]乙基]-2-叔丁基亚磺酰胺
[S(R)]-N-[(S)-[2-(二环己基膦)苯基](5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)甲基]-2-叔丁基亚磺酰胺
[S(R)]-N-[(S)-[3,5-二叔丁基-4-甲氧基苯基][2-(二环己基膦)苯基]甲基]-2-叔丁基亚磺酰胺
[S(R)]-N-[(1S)-1-[2-(二环己基膦)苯基]乙基]-N-甲基-2-叔丁基亚磺酰胺
[S(R)]-N-[(1S)-1-[2-(9-蒽基)苯基]-2-(二苯基膦)乙基]-N-甲基-2-叔丁基亚磺酰胺
[S(R)]-N-[(S)-[2-(二苯基膦)苯基]苯基甲基]-N-甲基-2-叔丁基亚磺酰胺
溶解性 | Soluble in DMSO (33 mg/mL), ethanol (1.7 mg/mL), and water (<1 mg/mL) at 25 °C. |
存贮条件 | 储存温度-20°C |
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 |