réservé à la recherche
AZD2281 (Olaparib) PARP inhibiteur
N° Cat.S1060
Structure chimique
Poids moléculaire: 434.46
Aller à
Contrôle qualité
Lot :
Pureté :
99.99%
99.99
Produits Souvent Utilisés Avec AZD2281 (Olaparib)
| Cibles apparentées | HDAC ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase eIF |
|---|---|
| Autre PARP Inhibiteurs | XAV-939 AZD5305 (Saruparib) PJ34 HCl AG-14361 Iniparib (BSI-201) G007-LK Pamiparib UPF 1069 A-966492 Stenoparib (E7449) |
Culture cellulaire, traitement et concentration de travail
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | PMID |
|---|---|---|---|---|---|---|
| Hep3B | Function Assay | 40 μM | 24 h | DMSO | Induces ROS production with DHMEQ | 25072752 |
| Huh7 | Growth Inhibition Assay | 40 μM | 72 h | DMSO | Synergistically inhibits cell growth with DHMEQ | 25072752 |
| Hep3B | Growth Inhibition Assay | 40 μM | 72 h | DMSO | Synergistically inhibits cell growth with DHMEQ | 25072752 |
| TE-6 | Function Assay | 5 μM | 24 h | DMSO | Increases in double strand breaks (DSBs) | 24219164 |
| TE-6 | Function Assay | 5 μM | 12 h | DMSO | Induces G2/M arrest | 24219164 |
| HT29 | Function Assay | 10 nM | 12 h | DMSO | Increases DNA double-strand breaks induced by SN-38 | 24577941 |
| HCT116 | Function Assay | 10 nM | 12 h | DMSO | Increases DNA double-strand breaks induced by SN-38 | 24577941 |
| RKO | Growth Inhibition Assay | 100 μM | 48 h | DMSO | Potentiates SN-38 cytotoxicity | 24577941 |
| C-1 | Growth Inhibition Assay | 100 μM | 48 h | DMSO | Potentiates SN-38 cytotoxicity | 24577941 |
| SW48 | Growth Inhibition Assay | 100 μM | 48 h | DMSO | Potentiates SN-38 cytotoxicity | 24577941 |
| LoVo | Growth Inhibition Assay | 100 μM | 48 h | DMSO | Potentiates SN-38 cytotoxicity | 24577941 |
| HT29 | Growth Inhibition Assay | 100 μM | 48 h | DMSO | Potentiates SN-38 cytotoxicity | 24577941 |
| SW1116 | Growth Inhibition Assay | 100 μM | 48 h | DMSO | Potentiates SN-38 cytotoxicity | 24577941 |
| HCT116 | Growth Inhibition Assay | 100 μM | 48 h | DMSO | Potentiates SN-38 cytotoxicity | 24577941 |
| RKO | Growth Inhibition Assay | 100 μM | 48 h | DMSO | IC50=5.9 μM | 24577941 |
| C-1 | Growth Inhibition Assay | 100 μM | 48 h | DMSO | IC50=7.6 μM | 24577941 |
| SW48 | Growth Inhibition Assay | 100 μM | 48 h | DMSO | IC50=9.5 μM | 24577941 |
| HCT-15 | Growth Inhibition Assay | 100 μM | 48 h | DMSO | IC50=10 μM | 24577941 |
| LoVo | Growth Inhibition Assay | 100 μM | 48 h | DMSO | IC50=13.4 μM | 24577941 |
| HT29 | Growth Inhibition Assay | 100 μM | 48 h | DMSO | IC50=14.7 μM | 24577941 |
| SW1116 | Growth Inhibition Assay | 100 μM | 48 h | DMSO | IC50=100 μM | 24577941 |
| HCT116 | Growth Inhibition Assay | 100 μM | 48 h | DMSO | IC50=2.5 μM | 24577941 |
| T47D | Growth Inhibition Assay | 5 day | IC50=9.6 μM | 23760496 | ||
| MCF7 | Growth Inhibition Assay | 5 day | IC50=5.8 μM | 23760496 | ||
| CAMA1 | Growth Inhibition Assay | 5 day | IC50=15.8 μM | 23760496 | ||
| SUM159 | Growth Inhibition Assay | 5 day | IC50=4.2 μM | 23760496 | ||
| SKBR3 | Growth Inhibition Assay | 5 day | IC50=11.1 μM | 23760496 | ||
| JIMT1 | Growth Inhibition Assay | 5 day | IC50=7.7 μM | 23760496 | ||
| BT474 | Growth Inhibition Assay | 5 day | IC50=19.8 μM | 23760496 | ||
| Hs578t(si) | Growth Inhibition Assay | 5 day | IC50=7.5 μM | 23760496 | ||
| Hs578t | Growth Inhibition Assay | 5 day | IC50=5.6 μM | 23760496 | ||
| HCC1937 | Growth Inhibition Assay | 5 day | IC50=12.6 μM | 23760496 | ||
| HCC1143 | Growth Inhibition Assay | 5 day | IC50=11.1 μM | 23760496 | ||
| BT20 | Growth Inhibition Assay | 5 day | IC50=7.7 μM | 23760496 | ||
| MDA-MB-468 | Growth Inhibition Assay | 5 day | IC50=5.0 μM | 23760496 | ||
| MDA-MB-231 | Growth Inhibition Assay | 5 day | IC50=6.9 μM | 23760496 | ||
| PC-9PTEN− | Growth Inhibition Assay | 20 μM | 144 h | IC50=6.52 μM | 23239809 | |
| PC-9 | Growth Inhibition Assay | 20 μM | 144 h | IC50=5.88 μM | 23239809 | |
| H1650PTEN+ | Growth Inhibition Assay | 20 μM | 144 h | IC50=50.83 μM | 23239809 | |
| H1650 | Growth Inhibition Assay | 20 μM | 144 h | IC50=15.47 μM | 23239809 | |
| Mouse ATM−/− ES Cells | Cytotoxic Assay | 2.5 μM | 20 h | Significantly inhibits cell survival | 23355489 | |
| Mouse H2AX−/− ES Cells | Cytotoxic Assay | 2.5 μM | 20 h | Significantly inhibits cell survival | 23355489 | |
| VCaP | Invasive Assay | 25 μM | 48 h | DMSO | Significantly reduces ERG-driven cell invasion | 21575865 |
| RWPE | Invasive Assay | 25 μM | 48 h | DMSO | Significantly reduces ERG-driven cell invasion | 21575865 |
| Z138 | Cytotoxic Assay | 5 μM | 96 h | DMSO | Slightly inhibits cell survival | 20124459 |
| JVM-2 | Cytotoxic Assay | 5 μM | 96 h | DMSO | Slightly inhibits cell survival | 20124459 |
| HBL-2 | Cytotoxic Assay | 5 μM | 96 h | DMSO | Slightly inhibits cell survival | 20124459 |
| UPN2 | Cytotoxic Assay | 5 μM | 96 h | DMSO | Slightly inhibits cell survival | 20124459 |
| BT | Cytotoxic Assay | 5 μM | 96 h | DMSO | Slightly inhibits cell survival | 20124459 |
| Granta-519 | Cytotoxic Assay | 5 μM | 96 h | DMSO | Slightly inhibits cell survival | 20124459 |
| L3 | Cytotoxic Assay | 5 μM | 96 h | DMSO | Significantly inhibits cell survival | 20124459 |
| T98G | Function Assay | 1 μM | 24 h | Enhances radiation-induced S-phase arrest | 18954712 | |
| HeLa | Function Assay | 1 μM | 24 h | Enhances radiation-induced S-phase arrest | 18954712 | |
| HeLa | Function Assay | 500 nM | 4 h | Causes a modest delay in rejoining of radiation-induced DNA breaks | 18954712 | |
| UVW | Cytotoxic Assay | 500 nM | 24 h | Increases radiation sensitivity | 18954712 | |
| U87-MG | Cytotoxic Assay | 1 μM | 24 h | Increases radiation sensitivity | 18954712 | |
| T98G | Cytotoxic Assay | 1 μM | 24 h | Increases radiation sensitivity | 18954712 | |
| U373-MG | Cytotoxic Assay | 1 μM | 24 h | Increases radiation sensitivity | 18954712 | |
| KB2P1.21 | Growth Inhibition Assay | 4 d | IC50=8907 nM | 18559613 | ||
| KB2P3.4 | Growth Inhibition Assay | 4 d | IC50=124 M | 18559613 | ||
| KP7.7 | Growth Inhibition Assay | 4 d | IC50=57 nM | 18559613 | ||
| KP6.3 | Growth Inhibition Assay | 4 d | IC50=10.428 μM | 18559613 | ||
| KP3.33 | Growth Inhibition Assay | 4 d | IC50=5.705 μM | 18559613 | ||
| Huh7 | Function Assay | 40 μM | 24 h | DMSO | Induces ROS production with DHMEQ | 25072752 |
| Hep3B | Function Assay | 40 μM | 24 h | DMSO | Induces cell autophagy with DHMEQ | 25072752 |
| Huh7 | Function Assay | 40 μM | 24 h | DMSO | Induces cell autophagy with DHMEQ | 25072752 |
| SGC-7901 | Growth Inhibition Assay | 30 μM | 48 h | DMSO | Block oxaliplatin-induced cell death | 25767076 |
| Sf9 | streptavidin-horseradish peroxidase-based luminescence assay | IC50=0.001 μM | 26546219 | |||
| T98G | immunofluorescence assay | IC50=0.0016 μM | 26469301 | |||
| G7 | immunofluorescence assay | IC50=0.0016 μM | 26469301 | |||
| HeLa | fluorescence assay | EC50=0.0025 μM | 24398383 | |||
| Sf9 | UV/Vis spectrophotometric analysis | IC50=0.00281 μM | 28601509 | |||
| Sf9 | streptavidin-horseradish peroxidase-based luminescence assay | IC50=0.003 μM | 26546219 | |||
| 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 | UV/Vis spectrophotometric analysis | IC50=0.00359 μM | 28601509 | |||
| SW620 | Ex vivo inhibition of PARP1 | IC50=0.006 μM | 18800822 | |||
| OVCAR8 | Binding affinity to PARP1 | IC50=0.006 μM | 29856625 | |||
| MDA-MB-436 | Cytotoxicity assay | CC50=0.0169 μM | 24815508 | |||
| 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 | |||
| MX1 | Cytotoxicity assay | EC50=0.0232 μM | 26652717 | |||
| MDA-MB-436 | CCK8 or SRB assay | IC50=0.0393 μM | 28692916 | |||
| MDA-MB-436 | Cytotoxicity assay | CC50=0.0432 μM | 23473053 | |||
| Jurkat | MTS assay in presence of 100 uM of temozolomide | EC50=0.06 μM | 23850199 | |||
| UWB1.289 | cell-titer glo assay | EC50=0.2 μM | 29856625 | |||
| VC8 | Cytotoxicity assay | CC50=0.201 μM | 23473053 | |||
| LoVo | Celltiter-Glo assay | GI50=0.237 μM | 26652717 | |||
| Capan1 | Cytotoxicity assay | EC50=0.259 μM | 26652717 | |||
| Capan1 | CCK8 or SRB assay | IC50=0.3993 μM | 28692916 | |||
| VC8 | CCK8 assay | CC50=0.456 μM | 29335205 | |||
| VC8 | Cytotoxicity assay | CC50=0.468 μM | 24815508 | |||
| VC8 | CCK8 or SRB assay | IC50=0.5656 μM | 28692916 | |||
| A2780 | SRB assay | IC50=1 μM | 24398383 | |||
| Sf9 | streptavidin-horseradish peroxidase-based luminescence assay | IC50=1.2 μM | 29856625 | |||
| Sf9 | streptavidin-horseradish peroxidase-based luminescence assay | IC50=1.7 μM | 26546219 | |||
| Sf9 | streptavidin-horseradish peroxidase-based luminescence assay | IC50=1.8 μM | 29856625 | |||
| 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 | |||
| Cliquez pour voir plus de données expérimentales sur les lignées cellulaires | ||||||
Informations chimiques, stockage et stabilité
| Poids moléculaire | 434.46 | Formule | C24H23FN4O3 |
Stockage (À partir de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 763113-22-0 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | Ku-0059436 | Smiles | C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F | ||
Solubilité
|
In vitro |
DMSO
: 125 mg/mL
(287.71 mM)
Chauffé avec un bain-marie à 50°C;
Ultrasonifié;
Water : Insoluble Ethanol : Insoluble |
Calculateur de molarité
Calculateur de dilution
Calculateur de poids moléculaire
|
In vivo |
|||||
Calculateur de formulation in vivo (Solution claire)
Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
mg/kg
g
μL
Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.
Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.
Mécanisme daction
| Fonctionnalités |
A potent PARP inhibitor (currently in late stage clinical trials).
|
|---|---|
| Targets/IC50/Ki |
PARP2
(Cell-free assay) 1 nM
PARP1
(Cell-free assay) 5 nM
|
| In vitro |
L'Olaparib (AZD2281) agirait contre les mutations BRCA1 ou BRCA2 et n'est pas sensible à la tankyrase-1 (IC50 >1 μM). Il pourrait abolir l'activité de PARP-1 à des concentrations de 30-100 nM dans les cellules SW620. Ce composé est hypersensible aux lignées cellulaires déficientes en BRCA1 (MDA-MB-463 et HCC1937), comparativement aux lignées cellulaires compétentes en BRCA1 et BRCA2 (Hs578T, MDA-MB-231 et T47D). Il est fortement sensible aux cellules KB2P en raison de la suppression de la réparation par excision de base par l'inhibition de PARP, ce qui peut entraîner la conversion des cassures simple brin en cassures double brin pendant la réplication de l'ADN, activant ainsi les voies de recombinaison dépendantes de BRCA2. |
| Kinase Assay |
Essai FlashPlate (essai de dépistage à 96 puits)
|
|
Dans les colonnes 1 à 10, 1 μL d'Olaparib (AZD2281) (dans du DMSO) est ajouté, et seulement 1 μL de DMSO est ajouté aux puits de contrôle positif (POS) et négatif (NEG) (colonnes 11 et 12, respectivement) d'une FlashPlate prétraitée. PARP-1 est diluée 1:40 dans un tampon (tampon B : 10 % de glycérol (v/v), 25 mM HEPES, 12,5 mM MgCl2, 50 mM KCl, 1 mM DTT, 0,01 % NP-40 (v/v), pH 7,6) et 40 μL sont ajoutés à l'ensemble des 96 puits (la concentration finale de PARP-1 dans l'essai est d'environ 1 ng/μL). La plaque est scellée et agitée à température ambiante pendant 15 min. Ensuite, 10 μL de mélange réactionnel positif (0,2 ng/μL d'oligonucléotide double brin [M3/M4] d'ADN par puits, 5 μM de NAD+ en concentration finale d'essai, et 0,075 μCi de 3H-NAD+ par puits) sont ajoutés aux puits appropriés (colonnes 1 à 11). Le mélange réactionnel négatif, dépourvu d'oligonucléotide d'ADN, est ajouté à la colonne 12 (avec la valeur moyenne du contrôle négatif utilisée comme arrière-plan). La plaque est à nouveau scellée et agitée pendant 60 min supplémentaires à température ambiante pour permettre à la réaction de se poursuivre. Ensuite, 50 μL d'acide acétique glacé (30 %) sont ajoutés à chaque puits pour arrêter la réaction, et la plaque est scellée et agitée pendant 60 min supplémentaires à température ambiante. Le signal tritié lié à la FlashPlate est ensuite déterminé en coups par minute (CPM) à l'aide du lecteur de plaque TopCount.
|
|
| In vivo |
L'Olaparib (AZD2281) (10 mg/kg, p.o.) en combinaison supprime significativement la croissance tumorale dans les xénogreffes SW620. Il montre une excellente réponse aux tumeurs mammaires Brca1-/-;p53-/- (50 mg/kg i.p. par jour), tandis qu'aucune réponse n'est observée aux tumeurs mammaires déficientes en HR Ecad-/-;p53-/-. Ce composé ne présente même pas de toxicité limitant la dose chez les souris porteuses de tumeurs. Il a été utilisé pour traiter les tumeurs mutées BRCA, telles que les cancers de l'ovaire, du sein et de la prostate. De plus, il montre une inhibition sélective des cellules tumorales déficientes en ATM (Ataxia Telangiectasia Mutated), ce qui indique qu'il s'agit d'un agent potentiel pour le traitement des tumeurs lymphoïdes mutantes ATM. |
Références |
|
Applications
| Méthodes | Biomarqueurs | Images | 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 |
Informations sur lessai clinique
(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Sponsor/Collaborateurs | Date de début | 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 |
Support technique
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