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
产品质控
批次：
纯度：
99.99%
99.99
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
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 |
|
25531448 | |
| Immunofluorescence | DNA damage γH2AX |
|
27686740 | |
| Growth inhibition assay | Cell viability |
|
25531448 | |
| ELISA | IL-8 GLP-1 |
|
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] |
|
|---|---|---|
| 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 |
|---|---|---|---|---|---|
| NCT05128734 | Not yet recruiting | Breast Cancer Triple Negative |
AHS Cancer Control Alberta |
July 1 2024 | Phase 2 |
| NCT05900895 | Not yet recruiting | Metastatic Breast Cancer |
Mary D Chamberlin|Dartmouth-Hitchcock Medical Center |
May 2024 | Phase 1 |
| NCT06377267 | Recruiting | Ovarian Cancer |
Vall d''Hebron Institute of Oncology |
February 6 2024 | Phase 2 |
| 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 |
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) | |||
|
体外溶解度 |
DMSO : 125 mg/mL ( (287.71 mM) Warmed with 50°C water bath; Ultrasonicated; ；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 |
|
体内溶解配方 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）
mg/kg
g
μL
只
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）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
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。
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