- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
- JAK/STAT
- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
- 化合物ライブラリー
- 抗体
- 新製品
- お問い合わせ
Olaparib (AZD2281)
別名：Ku-0059436
オラパリブ (Olaparib (AZD2281, KU0059436)) は選択的 PARP1/2 阻害剤であり、cell-free assay における IC50 はそれぞれ 5 nM および 1 nM です。タンキラーゼ-1 (Tankyrase-1) に対しては 1/300 の効果を示します。オラパリブは BRCA に変異をきたした細胞において、マイトファジー (mitophagy) に関連した顕著なオートファジー (mitophagy) を誘発します。
CAS No. 763113-22-0
文献中Selleckの製品使用例（1073）
製品安全説明書
現在のバッチを見る：
純度：
99.99%
99.99
Olaparib (AZD2281)と併用されることが多い化合物
Niraparib induces apoptosis and suppresses anti-apoptotic protein expression in KMCH-1 cells, while Olaparib has minimal impact on apoptosis induction in KMCH-1 cells.
Bezrookove V, et al. Cancers (Basel). 2021 Aug 31;13(17):4405.
Olaparib and Talazoparib are approved monotherapies for individuals with deleterious or suspected deleterious germline BRCA mutations and HER2-negative breast cancer.
Olaparib significantly inhibits cell survival in BRCA1 and BRCA2 mutant cell lines, while Velaparib does not induce cell death in these cell lines.
Olaparib and Rucaparib potently block the formation of poly-ADP-ribose (PAR) and demonstrate approximately similar capabilities in inducing PARP1 trapping in HeLa cells.
Olaparib and Paclitaxel combined with carboplatin enhance disease control and reduce the recurrence rate without extra toxic side effects in patients with ovarian cancer.
Zhang H, et al. Am J Transl Res. 2022 Jan 15;14(1):468-475. eCollection 2022.
Olaparib (AZD2281)関連製品
シグナル伝達経路
PARP阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| 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 | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | オラパリブ (Olaparib (AZD2281, KU0059436)) は選択的 PARP1/2 阻害剤であり、cell-free assay における IC50 はそれぞれ 5 nM および 1 nM です。タンキラーゼ-1 (Tankyrase-1) に対しては 1/300 の効果を示します。オラパリブは BRCA に変異をきたした細胞において、マイトファジー (mitophagy) に関連した顕著なオートファジー (mitophagy) を誘発します。 | ||||
|---|---|---|---|---|---|
| 特性 | A potent PARP inhibitor (currently in late stage clinical trials). | ||||
| Targets |
|
| In Vitro | ||||
| In vitro | Olaparib would act against BRCA1 or BRCA2 mutations. Olaparib is not sensitive to tankyrase-1 (IC50 >1 μM). Olaparib could ablate the PARP-1 activity at concentrations of 30-100 nM in SW620 cells. Olaparib is hypersensitive to BRCA1-deficient cell lines (MDA-MB-463 and HCC1937), compared with BRCA1- and BRCA2-proficient cell lines (Hs578T, MDA-MB-231, and T47D). [1] 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. [2] | |||
|---|---|---|---|---|
| Kinase Assay | FlashPlate assay (96-well screening assay) | |||
| To columns 1 through 10, 1 μL of Olaparib (in DMSO) is added, and 1 μL DMSO only is added to the positive (POS) and negative (NEG) control wells (columns 11 and 12, respectively) of a pretreated FlashPlate. PARP-1 is diluted 1:40 in buffer (buffer B: 10% glycerol (v/v), 25 mM HEPES, 12.5 mM MgCl2,50 mM KCl, 1 mM DTT, 0.01% NP-40 (v/v), pH 7.6) and 40 μL added to all 96 wells (final PARP-1 concentration in the assay is ~1 ng/μL). The plate is sealed and shaken at RT for 15 min. Following this, 10 μL of positive reaction mix (0.2 ng/μL of double-stranded oligonucleotide [M3/M4] DNA per well, 5 μM of NAD+ final assay concentration, and 0.075 μCi 3H-NAD+ per well) is added to the appropriate wells (columns 1-11). The negative reaction mix, lacking the DNA oligonucleotide, is added to column 12 (with the mean negative control value used as the background). The plate is resealed and shaken for a further 60 min at RT to allow the reaction to continue. Then, 50 μL of ice-cold acetic acid (30%) is added to each well to stop the reaction, and the plate is sealed and shaken for a further 60 min at RT. Tritiated signal bound to the FlashPlate is then determined in counts per minute (CPM) using the TopCount plate reader. | ||||
| 細胞実験 | 細胞株 | Breast cancer cell lines including SW620 colon, A2780 ovarian, HCC1937, Hs578T, MDA-MB-231, MDA-MB-436, and T47D | ||
| 濃度 | 1-300 nM | |||
| 反応時間 | 7-14 days | |||
| 実験の流れ | The cytotoxicity of Olaparib is measured by clonogenic assay. Olaparib is dissolved in DMSO and diluted by culture media before use. The cells are seeded in six well plates and left to attach overnight. Then Olaparib is added at various concentrations and the cells are incubated for 7-14 days. After that the surviving colonies are counted for calculating the IC50. |
|||
| 実験結果図 | Methods | Biomarkers | 結果図 | 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 | |
| In Vivo | ||
| In Vivo | Combining with temozolomide, Olaparib (10 mg/kg, p.o.) significantly suppresses tumor growth in SW620 xenografts. [1] Olaparib shows great response to Brca1-/-;p53-/- mammary tumors (50 mg/kg i.p. per day), while no responses to HR-deficient Ecad-/-;p53-/- mammary tumors. Olaparib even does not show dose-limiting toxicity in tumor-bearing mice. [3] Olaparib has been used to treat with BRCA mutated tumors, such as ovarian, breast and prostate cancers. Moreover, Olaparib shows selectively inhibition to ATM (Ataxia Telangiectasia Mutated)-deficient tumor cells, which indicates to be a potential agent for treating ATM mutant lymphoid tumors. [4] | |
|---|---|---|
| 動物実験 | 動物モデル | Brca1-/-;p53-/- mammary tumors are generated in K14cre;Brca1F/F;p53F/F mice. |
| 投与量 | 50 mg/kg | |
| 投与経路 | Administered via i.p. injection at 10 μL/g of body weight | |
| 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 |
化学情報
| 分子量 | 434.46 | 化学式 | C24H23FN4O3 |
| CAS No. | 763113-22-0 | SDF | Download Olaparib (AZD2281) SDFをダウンロードする |
| Smiles | C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F | ||
| 保管 | |||
|
In vitro |
DMSO : 87 mg/mL ( (200.24 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble Ethanol : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
技術サポート
ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。
他に質問がある場合は、お気軽にお問い合わせください。
* 必須
よくある質問（FAQ）
質問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.
質問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.
質問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.
Tags: Olaparib (AZD2281)を買う | Olaparib (AZD2281) ic50 | Olaparib (AZD2281)供給者 | Olaparib (AZD2281)を購入する | Olaparib (AZD2281)費用 | Olaparib (AZD2281)生産者 | オーダーOlaparib (AZD2281) | Olaparib (AZD2281)化学構造 | Olaparib (AZD2281)分子量 | Olaparib (AZD2281)代理店
納期 国内在庫品：受注日の翌日（15時までの受注分） ＊北海道、九州、沖縄への配送は受注日より２日以上 を要する場合あり 海外在庫品：受注後１〜２週間