solo para uso en investigación
AZD2281 (Olaparib) PARP inhibidor
Cat. No.S1060
Estructura química
Peso molecular: 434.46
Saltar a
Control de calidad
Lote:
Pureza:
99.99%
99.99
Productos que se suelen utilizar junto con AZD2281 (Olaparib)
| Dianas relacionadas | HDAC ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase eIF |
|---|---|
| Otros PARP Inhibidores | XAV-939 AZD5305 (Saruparib) PJ34 HCl AG-14361 Iniparib (BSI-201) G007-LK Pamiparib UPF 1069 A-966492 Stenoparib (E7449) |
Cultivo celular, tratamiento y concentración de trabajo
| Líneas celulares | Tipo de ensayo | Concentración | Tiempo de incubación | Formulación | Descripción de la actividad | 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 | |||
| Haga clic para ver más datos experimentales de líneas celulares | ||||||
Información química, almacenamiento y estabilidad
| Peso molecular | 434.46 | Fórmula | C24H23FN4O3 |
Almacenamiento (Desde la fecha de recepción) | |
|---|---|---|---|---|---|
| Nº CAS | 763113-22-0 | Descargar SDF | Almacenamiento de soluciones madre |
|
|
| Sinónimos | Ku-0059436 | Smiles | C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F | ||
Solubilidad
|
In vitro |
DMSO
: 125 mg/mL
(287.71 mM)
Calentado con baño de agua a 50°C;
Ultrasonido;
Water : Insoluble Ethanol : Insoluble |
Calculadora de Molaridad
Calculadora de Dilución
Calculadora de Peso Molecular
|
In vivo |
|||||
Calculadora de formulación in vivo (Solución clara)
Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)
mg/kg
g
μL
Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Resultados del cálculo:
Concentración de trabajo: mg/ml;
Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )
Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.
Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.
Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.
Mecanismo de acción
| Características |
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 |
Olaparib (AZD2281) actuaría contra las mutaciones BRCA1 o BRCA2 y no es sensible a la tankyrase-1 (IC50 >1 μM). Podría anular la actividad PARP-1 a concentraciones de 30-100 nM en células SW620. Este compuesto es hipersensible a las líneas celulares deficientes en BRCA1 (MDA-MB-463 y HCC1937), en comparación con las líneas celulares competentes en BRCA1 y BRCA2 (Hs578T, MDA-MB-231 y T47D). Es fuertemente sensible a las células KB2P debido a la supresión de la reparación por escisión de bases por la inhibición de PARP, lo que puede resultar en la conversión de roturas de cadena sencilla a roturas de doble cadena durante la replicación del ADN, activando así las vías de recombinación dependientes de BRCA2. |
| Ensayo de quinasa |
Ensayo FlashPlate (ensayo de cribado de 96 pocillos)
|
|
En las columnas 1 a 10, se añade 1 μL de Olaparib (AZD2281) (en DMSO), y solo se añade 1 μL de DMSO a los pocillos de control positivo (POS) y negativo (NEG) (columnas 11 y 12, respectivamente) de una FlashPlate pretratada. PARP-1 se diluye 1:40 en tampón (tampón B: 10% de glicerol (v/v), 25 mM de HEPES, 12,5 mM de MgCl2, 50 mM de KCl, 1 mM de DTT, 0,01% de NP-40 (v/v), pH 7,6) y se añaden 40 μL a los 96 pocillos (la concentración final de PARP-1 en el ensayo es de ~1 ng/μL). La placa se sella y se agita a temperatura ambiente durante 15 min. Después de esto, se añaden 10 μL de mezcla de reacción positiva (0,2 ng/μL de ADN de oligonucleótido de doble cadena [M3/M4] por pocillo, 5 μM de concentración final de NAD+ en el ensayo, y 0,075 μCi de 3H-NAD+ por pocillo) a los pocillos apropiados (columnas 1-11). La mezcla de reacción negativa, que carece del oligonucleótido de ADN, se añade a la columna 12 (utilizándose el valor medio del control negativo como fondo). La placa se vuelve a sellar y se agita durante otros 60 min a temperatura ambiente para permitir que la reacción continúe. Luego, se añaden 50 μL de ácido acético helado (30%) a cada pocillo para detener la reacción, y la placa se sella y se agita durante otros 60 min a temperatura ambiente. La señal tritiada unida a la FlashPlate se determina luego en recuentos por minuto (CPM) utilizando el lector de placas TopCount.
|
|
| In vivo |
Olaparib (AZD2281) (10 mg/kg, p.o.) en combinación suprime significativamente el crecimiento tumoral en xenoinjertos SW620. Muestra una gran respuesta a los tumores mamarios Brca1-/-;p53-/- (50 mg/kg i.p. por día), mientras que no hay respuestas a los tumores mamarios Ecad-/-;p53-/- deficientes en HR. Este compuesto incluso no muestra toxicidad limitante de la dosis en ratones con tumores. Se ha utilizado para tratar tumores con mutaciones BRCA, como los cánceres de ovario, mama y próstata. Además, muestra una inhibición selectiva de las células tumorales deficientes en ATM (Ataxia Telangiectasia Mutated), lo que indica que podría ser un agente potencial para el tratamiento de tumores linfoides mutantes de ATM. |
Referencias |
|
Aplicaciones
| Métodos | Biomarcadores | Imágenes | 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 |
Información del ensayo clínico
(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)
| Número NCT | Reclutamiento | Condiciones | Patrocinador/Colaboradores | Fecha de inicio | Fases |
|---|---|---|---|---|---|
| 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 |
Soporte técnico
Tel: +1-832-582-8158 Ext:3
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