Olaparib (AZD2281)
别名: Ku-0059436 中文名称：奥拉帕尼
Olaparib (AZD2281, KU0059436)是选择性的PARP1/2抑制剂，IC50为5 nM/1 nM，其对PARP1/2的作用比对Tankyrase-1效果高300倍。在BRCA突变的细胞中，Olaparib可以显著地诱导线粒体自噬相关的细胞自噬。
Olaparib (AZD2281) Chemical Structure
CAS: 763113-22-0
客户使用Selleck的Olaparib (AZD2281)发表文献1086篇
产品质控
常与Olaparib (AZD2281)一起在实验中被使用的化合物
在KMCH-1细胞中，Niraparib诱导凋亡并抑制抗凋亡蛋白的表达，而Olaparib对KMCH-1细胞诱导凋亡的影响最小。
Bezrookove V, et al. Cancers (Basel). 2021 Aug 31;13(17):4405.
Olaparib和Talazoparib被批准用于BRCA突变和HER2阴性乳腺癌患者的单药治疗。
Olaparib显著抑制BRCA1和BRCA2突变细胞系的细胞存活，而Velaparib不诱导这些细胞系的细胞死亡。
Olaparib和Rucaparib能有效阻断聚ADP核糖的形成，并在诱导HeLa细胞中PARP1捕获方面表现出相似的能力。
Olaparib和Paclitaxel联合Carboplatin可增强卵巢癌患者的疾病控制，降低复发率，且无额外毒副作用。
Zhang H, et al. Am J Transl Res. 2022 Jan 15;14(1):468-475. eCollection 2022.
Olaparib (AZD2281)相关产品
相关信号通路图
PARP抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| SGC-7901 | Growth Inhibition Assay | 30 μM | 48 h | Block oxaliplatin-induced cell death | 25767076 |
| Huh7 | Function Assay | 40 μM | 24 h | Induces cell autophagy with DHMEQ | 25072752 |
| Hep3B | Function Assay | 40 μM | 24 h | Induces cell autophagy with DHMEQ | 25072752 |
| Huh7 | Function Assay | 40 μM | 24 h | Induces ROS production with DHMEQ | 25072752 |
| U373-MG | Cytotoxic Assay | 1 μM | 24 h | Increases radiation sensitivity | 18954712 |
| T98G | Cytotoxic Assay | 1 μM | 24 h | Increases radiation sensitivity | 18954712 |
| U87-MG | Cytotoxic Assay | 1 μM | 24 h | Increases radiation sensitivity | 18954712 |
| UVW | Cytotoxic Assay | 500 nM | 24 h | Increases radiation sensitivity | 18954712 |
| HeLa | Function Assay | 500 nM | 4 h | Causes a modest delay in rejoining of radiation-induced DNA breaks | 18954712 |
| HeLa | Function Assay | 1 μM | 24 h | Enhances radiation-induced S-phase arrest | 18954712 |
| T98G | Function Assay | 1 μM | 24 h | Enhances radiation-induced S-phase arrest | 18954712 |
| L3 | Cytotoxic Assay | 5 μM | 96 h | Significantly inhibits cell survival | 20124459 |
| Granta-519 | Cytotoxic Assay | 5 μM | 96 h | Slightly inhibits cell survival | 20124459 |
| BT | Cytotoxic Assay | 5 μM | 96 h | Slightly inhibits cell survival | 20124459 |
| UPN2 | Cytotoxic Assay | 5 μM | 96 h | Slightly inhibits cell survival | 20124459 |
| HBL-2 | Cytotoxic Assay | 5 μM | 96 h | Slightly inhibits cell survival | 20124459 |
| JVM-2 | Cytotoxic Assay | 5 μM | 96 h | Slightly inhibits cell survival | 20124459 |
| Z138 | Cytotoxic Assay | 5 μM | 96 h | Slightly inhibits cell survival | 20124459 |
| RWPE | Invasive Assay | 25 μM | 48 h | Significantly reduces ERG-driven cell invasion | 21575865 |
| VCaP | Invasive Assay | 25 μM | 48 h | Significantly reduces ERG-driven cell invasion | 21575865 |
| Mouse H2AX−/− ES Cells | Cytotoxic Assay | 2.5 μM | 20 h | Significantly inhibits cell survival | 23355489 |
| Mouse ATM−/− ES Cells | Cytotoxic Assay | 2.5 μM | 20 h | Significantly inhibits cell survival | 23355489 |
| H1650 | Growth Inhibition Assay | 20 μM | 144 h | IC50=15.47 μM | 23239809 |
| H1650PTEN+ | Growth Inhibition Assay | 20 μM | 144 h | IC50=50.83 μM | 23239809 |
| PC-9 | Growth Inhibition Assay | 20 μM | 144 h | IC50=5.88 μM | 23239809 |
| PC-9PTEN− | Growth Inhibition Assay | 20 μM | 144 h | IC50=6.52 μM | 23239809 |
| HCT116 | Growth Inhibition Assay | 100 μM | 48 h | IC50=2.5 μM | 24577941 |
| SW1116 | Growth Inhibition Assay | 100 μM | 48 h | IC50=100 μM | 24577941 |
| HT29 | Growth Inhibition Assay | 100 μM | 48 h | IC50=14.7 μM | 24577941 |
| LoVo | Growth Inhibition Assay | 100 μM | 48 h | IC50=13.4 μM | 24577941 |
| HCT-15 | Growth Inhibition Assay | 100 μM | 48 h | IC50=10 μM | 24577941 |
| SW48 | Growth Inhibition Assay | 100 μM | 48 h | IC50=9.5 μM | 24577941 |
| C-1 | Growth Inhibition Assay | 100 μM | 48 h | IC50=7.6 μM | 24577941 |
| RKO | Growth Inhibition Assay | 100 μM | 48 h | IC50=5.9 μM | 24577941 |
| HCT116 | Growth Inhibition Assay | 100 μM | 48 h | Potentiates SN-38 cytotoxicity | 24577941 |
| SW1116 | Growth Inhibition Assay | 100 μM | 48 h | Potentiates SN-38 cytotoxicity | 24577941 |
| HT29 | Growth Inhibition Assay | 100 μM | 48 h | Potentiates SN-38 cytotoxicity | 24577941 |
| LoVo | Growth Inhibition Assay | 100 μM | 48 h | Potentiates SN-38 cytotoxicity | 24577941 |
| SW48 | Growth Inhibition Assay | 100 μM | 48 h | Potentiates SN-38 cytotoxicity | 24577941 |
| C-1 | Growth Inhibition Assay | 100 μM | 48 h | Potentiates SN-38 cytotoxicity | 24577941 |
| RKO | Growth Inhibition Assay | 100 μM | 48 h | Potentiates SN-38 cytotoxicity | 24577941 |
| HCT116 | Function Assay | 10 nM | 12 h | Increases DNA double-strand breaks induced by SN-38 | 24577941 |
| HT29 | Function Assay | 10 nM | 12 h | Increases DNA double-strand breaks induced by SN-38 | 24577941 |
| TE-6 | Function Assay | 5 μM | 12 h | Induces G2/M arrest | 24219164 |
| TE-6 | Function Assay | 5 μM | 24 h | Increases in double strand breaks (DSBs) | 24219164 |
| Hep3B | Growth Inhibition Assay | 40 μM | 72 h | Synergistically inhibits cell growth with DHMEQ | 25072752 |
| Huh7 | Growth Inhibition Assay | 40 μM | 72 h | Synergistically inhibits cell growth with DHMEQ | 25072752 |
| Hep3B | Function Assay | 40 μM | 24 h | Induces ROS production with DHMEQ | 25072752 |
| KP3.33 | Growth Inhibition Assay | 4 d | IC50=5.705 μM | 18559613 | |
| KP6.3 | Growth Inhibition Assay | 4 d | IC50=10.428 μM | 18559613 | |
| KP7.7 | Growth Inhibition Assay | 4 d | IC50=57 nM | 18559613 | |
| KB2P3.4 | Growth Inhibition Assay | 4 d | IC50=124 M | 18559613 | |
| KB2P1.21 | Growth Inhibition Assay | 4 d | IC50=8907 nM | 18559613 | |
| MDA-MB-231 | Growth Inhibition Assay | 5 day | IC50=6.9 μM | 23760496 | |
| MDA-MB-468 | Growth Inhibition Assay | 5 day | IC50=5.0 μM | 23760496 | |
| BT20 | Growth Inhibition Assay | 5 day | IC50=7.7 μM | 23760496 | |
| HCC1143 | Growth Inhibition Assay | 5 day | IC50=11.1 μM | 23760496 | |
| HCC1937 | Growth Inhibition Assay | 5 day | IC50=12.6 μM | 23760496 | |
| Hs578t | Growth Inhibition Assay | 5 day | IC50=5.6 μM | 23760496 | |
| Hs578t(si) | Growth Inhibition Assay | 5 day | IC50=7.5 μM | 23760496 | |
| BT474 | Growth Inhibition Assay | 5 day | IC50=19.8 μM | 23760496 | |
| JIMT1 | Growth Inhibition Assay | 5 day | IC50=7.7 μM | 23760496 | |
| SKBR3 | Growth Inhibition Assay | 5 day | IC50=11.1 μM | 23760496 | |
| SUM159 | Growth Inhibition Assay | 5 day | IC50=4.2 μM | 23760496 | |
| CAMA1 | Growth Inhibition Assay | 5 day | IC50=15.8 μM | 23760496 | |
| MCF7 | Growth Inhibition Assay | 5 day | IC50=5.8 μM | 23760496 | |
| T47D | Growth Inhibition Assay | 5 day | IC50=9.6 μM | 23760496 | |
| Sf9 | streptavidin-horseradish peroxidase-based luminescence assay | IC50=1.8 μM | 29856625 | ||
| Sf9 | streptavidin-horseradish peroxidase-based luminescence assay | IC50=1.7 μM | 26546219 | ||
| Sf9 | streptavidin-horseradish peroxidase-based luminescence assay | IC50=1.2 μM | 29856625 | ||
| A2780 | SRB assay | IC50=1 μM | 24398383 | ||
| VC8 | CCK8 or SRB assay | IC50=0.5656 μM | 28692916 | ||
| VC8 | Cytotoxicity assay | CC50=0.468 μM | 24815508 | ||
| VC8 | CCK8 assay | CC50=0.456 μM | 29335205 | ||
| Capan1 | CCK8 or SRB assay | IC50=0.3993 μM | 28692916 | ||
| Capan1 | Cytotoxicity assay | EC50=0.259 μM | 26652717 | ||
| LoVo | Celltiter-Glo assay | GI50=0.237 μM | 26652717 | ||
| VC8 | Cytotoxicity assay | CC50=0.201 μM | 23473053 | ||
| UWB1.289 | cell-titer glo assay | EC50=0.2 μM | 29856625 | ||
| Jurkat | MTS assay in presence of 100 uM of temozolomide | EC50=0.06 μM | 23850199 | ||
| MDA-MB-436 | Cytotoxicity assay | CC50=0.0432 μM | 23473053 | ||
| MDA-MB-436 | CCK8 or SRB assay | IC50=0.0393 μM | 28692916 | ||
| MX1 | Cytotoxicity assay | EC50=0.0232 μM | 26652717 | ||
| SKOV3 | Inhibition of PARP1/PARP2 | IC50=0.0209 μM | 23473053 | ||
| SKOV3 | Inhibition of PARP1/PARP2 | IC50=0.0209 μM | 23473053 | ||
| SKOV3 | Inhibition of PARP1/PARP2 | IC50=0.0209 μM | 23473053 | ||
| MDA-MB-436 | Cytotoxicity assay | CC50=0.0169 μM | 24815508 | ||
| OVCAR8 | Binding affinity to PARP1 | IC50=0.006 μM | 29856625 | ||
| SW620 | Ex vivo inhibition of PARP1 | IC50=0.006 μM | 18800822 | ||
| Sf9 | UV/Vis spectrophotometric analysis | IC50=0.00359 μM | 28601509 | ||
| LoVo | Inhibition of PARP | EC50=0.00357 μM | 26652717 | ||
| LoVo | Inhibition of PARP | EC50=0.00357 μM | 26652717 | ||
| LoVo | Inhibition of PARP | EC50=0.00357 μM | 26652717 | ||
| Sf9 | streptavidin-horseradish peroxidase-based luminescence assay | IC50=0.003 μM | 26546219 | ||
| Sf9 | UV/Vis spectrophotometric analysis | IC50=0.00281 μM | 28601509 | ||
| HeLa | fluorescence assay | EC50=0.0025 μM | 24398383 | ||
| G7 | immunofluorescence assay | IC50=0.0016 μM | 26469301 | ||
| T98G | immunofluorescence assay | IC50=0.0016 μM | 26469301 | ||
| Sf9 | streptavidin-horseradish peroxidase-based luminescence assay | IC50=0.001 μM | 26546219 | ||
| Sf9 | streptavidin-horseradish peroxidase-based luminescence assay | IC50=1.8 μM | 26546219 | ||
| Sf9 | streptavidin-horseradish peroxidase-based luminescence assay | IC50=1.9 μM | 26546219 | ||
| DLD-1 TOPFlash/EF1a Renilla reporter | Steady-Glo Luciferase assay | IC50=3 μM | 26546219 | ||
| DLD-1 TOPFlash/EF1a Renilla reporter | Steady-Glo Luciferase assay | IC50=3 μM | 26546219 | ||
| UWB1.289 | cell-titer glo assay | EC50=4.8 μM | 29856625 | ||
| HCC1937 | MTT assay | IC50=4.97 μM | 28763648 | ||
| MRC5 | Cytotoxicity assay | EC50=5.83 μM | 26652717 | ||
| Capan1 | SRB assay | IC50=6.3 μM | 24398383 | ||
| MDA-MB-231 | MTT assay | IC50=7.92 μM | 28601509 | ||
| MEF | cell-titer glo assay | EC50=8.5 μM | 29856625 | ||
| HCC1937 | MTT assay | IC50=8.65 μM | 28601509 | ||
| V79 | Cytotoxicity assay | CC50=8.985 μM | 24815508 | ||
| V79 | Cytotoxicity assay | CC50=10 μM | 23473053 | ||
| H23 | MTT assay | IC50=10 μM | 24521039 | ||
| V79 | CCK8 or SRB assay | IC50=10 μM | 28692916 | ||
| HCC1937 | SRB assay | IC50=10.3 μM | 24398383 | ||
| H460 | MTT assay | IC50=12 μM | 24521039 | ||
| MEF | cell-titer glo assay | EC50=14.6 μM | 29856625 | ||
| HCT116 | MTT assay | IC50=15.13 μM | 28763648 | ||
| Jurkat | MTS assay | EC50=16 μM | 23850199 | ||
| NCI-H1792 | MTT assay | IC50=16 μM | 24521039 | ||
| NCI-H1693 | MTT assay | IC50=19 μM | 24521039 | ||
| NCI-H1703 | MTT assay | IC50=20 μM | 24521039 | ||
| NCI-H2023 | MTT assay | IC50=20 μM | 24521039 | ||
| U937 | MTT assay | IC50=21.81 μM | 28601509 | ||
| NCI-H1944 | MTT assay | IC50=25 μM | 24521039 | ||
| H441 | MTT assay | IC50=28 μM | 24521039 | ||
| A549 | MTT assay | IC50=28 μM | 24521039 | ||
| NCI-H1355 | MTT assay | IC50=33 μM | 24521039 | ||
| NCI-H2030 | MTT assay | IC50=34 μM | 24521039 | ||
| MCF7 | MTT assay | IC50=35.24 μM | 28601509 | ||
| NCI-H1568 | MTT assay | IC50=36 μM | 24521039 | ||
| MCF7 | MTT assay | IC50=36.24 μM | 28763648 | ||
| NCI-H2122 | MTT assay | IC50=38 μM | 24521039 | ||
| MDA-MB-231 | MTT assay | IC50=39.51 μM | 28601509 | ||
| A2780/DX | SRB assay | IC50=41.9 μM | 24398383 | ||
| MEF | cell-titer glo assay | EC50=49.6 μM | 29856625 | ||
| NCI-H322M | MTT assay | IC50=50 μM | 24521039 | ||
| T47D | MTT assay | IC50=50 μM | 28601509 | ||
| HCC827 | MTT assay | IC50=50 μM | 28601509 | ||
| MCF10A | MTT assay | IC50=50 μM | 28601509 | ||
| HeLa | MTT assay | IC50=50 μM | 28601509 | ||
| K562 | MTT assay | IC50=50 μM | 28601509 | ||
| Raji | MTT assay | IC50=50 μM | 28601509 | ||
| COLO-800 | Growth Inhibition Assay | IC50=0.44164 μM | SANGER | ||
| EoL-1- | Growth Inhibition Assay | IC50=0.56446 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=0.91556 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=1.11408 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=1.25347 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=1.33341 μM | SANGER | ||
| MHH-ES-1 | Growth Inhibition Assay | IC50=1.62067 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=1.72414 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=2.20699 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=2.27534 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=2.44568 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=2.84173 μM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=2.88189 μM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=3.51696 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=3.60058 μM | SANGER | ||
| MC-IXC | Growth Inhibition Assay | IC50=3.63393 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=3.65448 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=3.73103 μM | SANGER | ||
| NCI-H510A | Growth Inhibition Assay | IC50=3.82724 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=3.86958 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=4.13334 μM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=4.2529 μM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=4.3586 μM | SANGER | ||
| KASUMI-1 | Growth Inhibition Assay | IC50=4.40109 μM | SANGER | ||
| LU-139 | Growth Inhibition Assay | IC50=4.75829 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=4.80908 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=4.89443 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=5.08072 μM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=5.12055 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=5.15244 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=5.20006 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=5.51389 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=5.56856 μM | SANGER | ||
| NCI-H1048 | Growth Inhibition Assay | IC50=5.97273 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=6.022 μM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=6.03577 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=6.09137 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=6.33974 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=6.49683 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=6.5109 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=6.64039 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=6.77424 μM | SANGER | ||
| NY | Growth Inhibition Assay | IC50=6.94605 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=7.10433 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=7.17494 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=7.31861 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=7.48417 μM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=7.72173 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=7.76175 μM | SANGER | ||
| 5637 | Growth Inhibition Assay | IC50=7.9286 μM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=7.94016 μM | SANGER | ||
| HOS | Growth Inhibition Assay | IC50=8.23007 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=8.2358 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=8.30088 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=8.5554 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=8.68988 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=8.70921 μM | SANGER | ||
| NCI-H69 | Growth Inhibition Assay | IC50=9.90961 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=11.2208 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=11.2947 μM | SANGER | ||
| SF539 | Growth Inhibition Assay | IC50=11.4889 μM | SANGER | ||
| HuO-3N1 | Growth Inhibition Assay | IC50=11.5796 μM | SANGER | ||
| NCI-H1651 | Growth Inhibition Assay | IC50=12.3115 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=12.376 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=12.4609 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=13.1095 μM | SANGER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=13.2856 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=13.445 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=13.7814 μM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=13.8475 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition Assay | IC50=13.9347 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=14.0637 μM | SANGER | ||
| TI-73 | Growth Inhibition Assay | IC50=14.2356 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=15.5716 μM | SANGER | ||
| D-247MG | Growth Inhibition Assay | IC50=15.593 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=15.6097 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=15.6522 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=16.752 μM | SANGER | ||
| Mo-T | Growth Inhibition Assay | IC50=17.0849 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=17.1543 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=17.1827 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=17.7054 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=17.8728 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=18.1316 μM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=18.7414 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=18.7595 μM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=19.0489 μM | SANGER | ||
| L-428 | Growth Inhibition Assay | IC50=19.559 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=19.572 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=19.5747 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=19.5972 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=19.915 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=19.9967 μM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=20.2219 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=20.2615 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=20.5334 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=21.1613 μM | SANGER | ||
| A2058 | Growth Inhibition Assay | IC50=21.4477 μM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=21.9051 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=21.975 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=22.0651 μM | SANGER | ||
| JVM-2 | Growth Inhibition Assay | IC50=22.2983 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=22.7312 μM | SANGER | ||
| MKN28 | Growth Inhibition Assay | IC50=22.9015 μM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=23.741 μM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=24.0008 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=24.3337 μM | SANGER | ||
| 769-P | Growth Inhibition Assay | IC50=24.8466 μM | SANGER | ||
| HEC-1 | Growth Inhibition Assay | IC50=25.445 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=25.5331 μM | SANGER | ||
| 8505C | Growth Inhibition Assay | IC50=26.4977 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=26.7176 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=26.7648 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=27.1271 μM | SANGER | ||
| OVCAR-8 | Growth Inhibition Assay | IC50=27.1539 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=27.54 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=28.047 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=28.5096 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=28.5651 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=28.9204 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=29.868 μM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=29.993 μM | SANGER | ||
| HCT-116 | Growth Inhibition Assay | IC50=30.0548 μM | SANGER | ||
| S-117 | Growth Inhibition Assay | IC50=31.2257 μM | SANGER | ||
| NCI-H1693 | Growth Inhibition Assay | IC50=33.6542 μM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=33.9976 μM | SANGER | ||
| HT-29 | Growth Inhibition Assay | IC50=34.6032 μM | SANGER | ||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=34.7491 μM | SANGER | ||
| CAL-51 | Growth Inhibition Assay | IC50=35.0709 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=35.2425 μM | SANGER | ||
| SCH | Growth Inhibition Assay | IC50=36.4174 μM | SANGER | ||
| SK-MEL-24 | Growth Inhibition Assay | IC50=36.9044 μM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=38.7216 μM | SANGER | ||
| BALL-1 | Growth Inhibition Assay | IC50=39.2129 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=39.329 μM | SANGER | ||
| GI-1 | Growth Inhibition Assay | IC50=39.8647 μM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=39.9139 μM | SANGER | ||
| A673 | Growth Inhibition Assay | IC50=41.0343 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=43.394 μM | SANGER | ||
| GP5d | Growth Inhibition Assay | IC50=44.0666 μM | SANGER | ||
| MFM-223 | Growth Inhibition Assay | IC50=44.1228 μM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=44.2643 μM | SANGER | ||
| C8166 | Growth Inhibition Assay | IC50=45.0822 μM | SANGER | ||
| LU-99A | Growth Inhibition Assay | IC50=46.1322 μM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=46.1785 μM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=47.0998 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=47.1007 μM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=47.5069 μM | SANGER | ||
| DJM-1 | Growth Inhibition Assay | IC50=47.5413 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=47.6357 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=48.3072 μM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=48.4633 μM | SANGER | ||
| NCI-H1573 | Growth Inhibition Assay | IC50=49.4462 μM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=49.7411 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=49.9222 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Olaparib (AZD2281, KU0059436)是选择性的PARP1/2抑制剂，IC50为5 nM/1 nM，其对PARP1/2的作用比对Tankyrase-1效果高300倍。在BRCA突变的细胞中，Olaparib可以显著地诱导线粒体自噬相关的细胞自噬。 | ||||
|---|---|---|---|---|---|
| 特性 | Olaparib是第一批PARP抑制剂之一。 | ||||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | Olaparib是PARP抑制剂，也作用于BRCA1或BRCA2突变。Olaparib对端锚(聚合)酶-1作用效果不大，IC50值大于1 μM。Olaparib浓度为30-100 nM作用于SW620细胞，使PARP-1失活。与BRCA1和BRCA2充足细胞系(Hs578T,MDA-MB-231,T47D)相比，BRCA1缺陷细胞系(MDA-MB-463和HCC1937)对Olaparib过分敏感[1] Olaparib抑制PARP，阻断碱基切除修复，导致KB2P细胞对Olaparib强烈敏感。结果导致在DNA复制时由单链断裂转变为双链断裂，由此激活BRCA2依赖的重组途径。[2] |
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|---|---|---|---|---|
| 激酶实验 | 体外独立酶实验 | |||
| 通过PARP-1实验测定PARP-2抑制活性，实验在96孔板上进行，PARP-2特定抗体与重组PARP-2蛋白结合。加入3H-NAD+DNA测定PARP-2活性。 冲洗后，加入闪烁剂测定3H-渗透的核糖基化。通过AlphaScreen实验测定端锚聚合酶-1, 实验中HIS标签重组TANK-1蛋白和生物素化的NAD+ 在384孔Proxi板上温育。 加入Alpha 磁珠，与HIS和生物素化的标签结合，产生邻近信号，测定信号消失的比例来计算TANK-1抑制活性。 | ||||
| 细胞实验 | 细胞系 | 胸腺癌细胞系SW620结肠, A2780卵巢,HCC1937,Hs578T,MDA-MB-231,MDA-MB-436,和T47D | ||
| 浓度 | 1到300 nM | |||
| 孵育时间 | 7-14天 | |||
| 方法 | 通过成株实验测定Olaparib毒性。Olaparib溶于DMSO中，用培养基稀释。细胞接种在六孔板上，过夜使粘附。然后加入不同浓度Olaparib，温育7-14天。计算存活菌落，测定IC50值。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western Blot | DR5/CHOP γH2AX/H2AX pATM 53BP1 NF-kB pS6/S6 |
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25531448 | |
| Immunofluorescence | DNA damage γH2AX |
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27686740 | |
| Growth inhibition assay | Cell viability |
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25531448 | |
| ELISA | IL-8 GLP-1 |
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28456021 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 |
Olaparib有效作用于Brca1-/-;p53-/- 乳腺肿瘤 (每天按50 mg/kg剂量腹腔注射),但是对 HR缺陷的Ecad-/-;p53-/-乳腺肿瘤没有效果。Olaparib作用于携带肿瘤的鼠没有剂量限制毒性。[3] Olaparib已经用于治疗BRCA突变的肿瘤, 比如卵巢癌，胸腺癌，前列腺癌。此外，Olaparib抑制ATM缺陷的肿瘤细胞具有选择性，说明Olaparib可作为治疗ATM突变的淋巴肿瘤的潜在试剂。[4] |
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|---|---|---|
| 动物实验 | Animal Models | 携带Brca1-/-;p53-/-乳腺癌的 K14cre;Brca1F/F;p53F/F鼠 |
| Dosages | 50 mg/kg | |
| Administration | 按10 μL/g剂量腹腔注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05900895 | Not yet recruiting | Metastatic Breast Cancer |
Dickinson|Dartmouth-Hitchcock Medical Center |
December 2023 | Phase 1 |
| NCT06065059 | Recruiting | Breast Cancer|Ovarian Cancer|Pancreas Cancer|Prostate Cancer|BRCA1 Mutation|BRCA-Mutated Ovarian Carcinoma|BRCA-Associated Breast Carcinoma|HRD Positive Advanced Ovarian Cancer |
Tango Therapeutics Inc. |
December 8 2023 | Phase 1|Phase 2 |
| NCT05128734 | Not yet recruiting | Breast Cancer Triple Negative |
AHS Cancer Control Alberta |
December 1 2023 | Phase 2 |
| NCT05887609 | Recruiting | Ovary Cancer|Peritoneal Cancer|Fallopian Tube Cancer |
University of Colorado Denver|ImmunoGen Inc. |
October 3 2023 | Phase 2 |
化学信息&溶解度
| 分子量 | 434.46 | 分子式 | C24H23FN4O3 |
| CAS号 | 763113-22-0 | SDF | Download Olaparib (AZD2281) SDF |
| Smiles | C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 87 mg/mL ( (200.24 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
* 必填项
常见问题及建议解决方法
问题 1:
How to prepare the solution of the compound (S1060) for in vivo study?
回答：
We recommend the following formulation: 4% DMSO+30% PEG300+ 66%H2O. It is a clear solution and can be used for IP injection.
问题 2:
I saw that the solubility of the compound for in vivo on the website had been changed, why the change has been made?
回答：
For the formulation for in vivo, the compound dissolving in 15% Captisol (former solubility) is a suspension, and it is fine for oral gavage. And now, dissolving in 4% DMSO+30% PEG 300+ddH2O is a clear solution, and is for injection.
问题 3:
How long can the chemical compound be stable in DMEM at 4 °C?
回答：
The compound is stable in DMEM at 4 degree for one week.
