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AZD2281 (Olaparib) PARP remmer
Cat.Nr.S1060
Chemische structuur
Moleculair gewicht: 434.46
Ga naar
Kwaliteitscontrole
Batch:
Zuiverheid:
99.99%
99.99
Producten Vaak Samen Gebruikt Met AZD2281 (Olaparib)
| Gerelateerde doelwitten | HDAC ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase eIF |
|---|---|
| Overige PARP Inhibitoren | XAV-939 AZD5305 (Saruparib) PJ34 HCl AG-14361 Iniparib (BSI-201) G007-LK Pamiparib UPF 1069 A-966492 Stenoparib (E7449) |
Celkweek, behandeling & werkconcentratie
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | 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 | |||
| Klik om meer experimentele gegevens over de cellijn te bekijken | ||||||
Chemische informatie, Opslag en Stabiliteit
| Moleculair gewicht | 434.46 | Formule | C24H23FN4O3 |
Opslag (Vanaf de ontvangstdatum) | |
|---|---|---|---|---|---|
| CAS-nr. | 763113-22-0 | SDF downloaden | Opslag van stamoplossingen |
|
|
| Synoniemen | Ku-0059436 | Smiles | C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F | ||
Oplosbaarheid
|
In vitro |
DMSO
: 125 mg/mL
(287.71 mM)
Verwarmd met 50°C waterbad;
Geultrasoneerd;
Water : Insoluble Ethanol : Insoluble |
Molariteitscalculator
Verdunningscalculator
Moleculair gewicht calculator
|
In vivo |
|||||
In vivo Formuleringscalculator (Heldere oplossing)
Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)
mg/kg
g
μL
Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH2O, mengen en helder maken.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.
Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
Werkingsmechanisme
| Kenmerken |
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) zou werken tegen BRCA1- of BRCA2-mutaties en is niet gevoelig voor tankyrase-1 (IC50 >1 μM). Het zou de PARP-1 activiteit kunnen ablateren bij concentraties van 30-100 nM in SW620-cellen. Deze verbinding is overgevoelig voor BRCA1-deficiënte cellijnen (MDA-MB-463 en HCC1937), vergeleken met BRCA1- en BRCA2-efficiënte cellijnen (Hs578T, MDA-MB-231 en T47D). Het is sterk gevoelig voor KB2P-cellen door onderdrukking van base-excisieherstel door PARP-remming, wat kan resulteren in de omzetting van enkelstrengsbreuken naar dubbelstrengsbreuken tijdens DNA-replicatie, waardoor BRCA2-afhankelijke recombinatiepaden worden geactiveerd. |
| Kinase Assay |
FlashPlate assay (96-wells screening assay)
|
|
Aan kolommen 1 tot en met 10 wordt 1 μL Olaparib (AZD2281) (in DMSO) toegevoegd, en alleen 1 μL DMSO wordt toegevoegd aan de positieve (POS) en negatieve (NEG) controleputjes (kolommen 11 en 12, respectievelijk) van een voorbehandelde FlashPlate. PARP-1 wordt 1:40 verdund 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) en 40 μL wordt toegevoegd aan alle 96 putjes (finale PARP-1 concentratie in de assay is ~1 ng/μL). De plaat wordt afgedicht en 15 min. geschud bij RT. Hierna wordt 10 μL positieve reactiemix (0,2 ng/μL dubbelstrengs oligonucleotide [M3/M4] DNA per putje, 5 μM NAD+ finale assayconcentratie, en 0,075 μCi 3H-NAD+ per putje) toegevoegd aan de geschikte putjes (kolommen 1-11). De negatieve reactiemix, zonder het DNA-oligonucleotide, wordt toegevoegd aan kolom 12 (met de gemiddelde negatieve controlewaarde gebruikt als achtergrond). De plaat wordt opnieuw afgedicht en nog eens 60 min. geschud bij RT om de reactie te laten doorgaan. Vervolgens wordt 50 μL ijskoude azijnzuur (30%) aan elk putje toegevoegd om de reactie te stoppen, en de plaat wordt afgedicht en nog eens 60 min. geschud bij RT. Het getritieerde signaal gebonden aan de FlashPlate wordt vervolgens bepaald in counts per minute (CPM) met behulp van de TopCount plaatlezer.
|
|
| In vivo |
Olaparib (AZD2281) (10 mg/kg, p.o.) in combinatie onderdrukt significant de tumorgroei in SW620 xenografts. Het vertoont een goede respons op Brca1-/-;p53-/- mammatumoren (50 mg/kg i.p. per dag), terwijl er geen respons is op HR-deficiënte Ecad-/-;p53-/- mammatumoren. Deze verbinding vertoont zelfs geen dosisbeperkende toxiciteit bij tumorhoudende muizen. Het is gebruikt voor de behandeling van tumoren met BRCA-mutaties, zoals eierstok-, borst- en prostaatkanker. Bovendien vertoont het een selectieve remming van ATM (Ataxia Telangiectasia Mutated)-deficiënte tumorcellen, wat erop wijst dat het een potentieel middel is voor de behandeling van ATM-mutante lymfoïde tumoren. |
Referenties |
|
Toepassingen
| Methoden | Biomarkers | Afbeeldingen | 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 |
Informatie klinische proef
(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)
| NCT-nummer | Rekrutering | Aandoeningen | Sponsor/Medewerkers | Startdatum | Fasen |
|---|---|---|---|---|---|
| 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 |
Technische ondersteuning
Tel: +1-832-582-8158 Ext:3
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