- Bioactive Compounds
- By Signaling Pathways
- 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
- DNA Damage/DNA Repair
- Compound Libraries
- Antibodies
- Bioreagents
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- Protein Assay
- Protein A/G Magnetic Beads for IP
- Anti-Flag magnetic beads
- Anti-Flag Affinity Gel
- Anti-Myc magnetic beads
- Anti-HA magnetic beads
- Magnetic Separator
- Poly DYKDDDDK Tag Peptide lyophilized powder
- Protease Inhibitor Cocktail
- Protease Inhibitor Cocktail (EDTA-Free, 100X in DMSO)
- Phosphatase Inhibitor Cocktail (2 Tubes, 100X)
- Cell Biology
- Cell Counting Kit-8 (CCK-8)
- Animal Experiment
- Mouse Direct PCR Kit (For Genotyping)
- New Products
- Contact Us
-
Australia
-
Austria
-
Belgium
-
Canada
-
China
-
Czech Republic
-
Denmark
-
Finland
-
France
-
Germany
-
Greece
-
Hong Kong
-
Hungary
-
Iceland
-
India
-
Ireland
-
Israel
-
Italy
-
Japan
-
Korea
-
Luxembourg
-
Malaysia
-
Netherlands
-
New Zealand
-
Norway
-
Poland
-
Qatar
-
Romania
-
Saudi Arabia
-
Singapore
-
Spain
-
Sweden
-
Switzerland
-
Taiwan
-
Turkey
-
United Kingdom
-
United States
-
Other Countries
Olaparib (AZD2281)
Synonyms: Ku-0059436
Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.
Olaparib (AZD2281) Chemical Structure
CAS No. 763113-22-0
Purity & Quality Control
Batch:
Purity:
99.99%
99.99
Olaparib (AZD2281) Related Products
| Related Targets | PARP1 PARP2 PARP3 Tankyrase-1 Tankyrase-2 PARP14 PARP7 TNKS1 TNKS2 | Click to Expand |
|---|---|---|
| Related Products | XAV-939 Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) A-966492 G007-LK UPF 1069 AZD2461 Pamiparib ME0328 3-Aminobenzamide NMS-P118 Stenoparib (E7449) NVP-TNKS656 WIKI4 Benzamide BGP-15 2HCl NU1025 BYK204165 Fluzoparib (SHR-3162) Picolinamide | Click to Expand |
| Related Compound Libraries | FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library | Click to Expand |
Signaling Pathway
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | 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 | |||
| Click to View More Cell Line Experimental Data | ||||||
Biological Activity
| Description | Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations. | ||||
|---|---|---|---|---|---|
| Features | 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. | ||||
| Cell Research | Cell lines | Breast cancer cell lines including SW620 colon, A2780 ovarian, HCC1937, Hs578T, MDA-MB-231, MDA-MB-436, and T47D | ||
| Concentrations | 1-300 nM | |||
| Incubation Time | 7-14 days | |||
| Method | 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. |
|||
| Experimental Result Images | Methods | Biomarkers | 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 | |
| In Vivo | ||
| In vivo | Olaparib (10 mg/kg, p.o.) in Combination 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] |
|
|---|---|---|
| Animal Research | Animal Models | Brca1-/-;p53-/- mammary tumors are generated in K14cre;Brca1F/F;p53F/F mice. |
| Dosages | 50 mg/kg | |
| Administration | Administered via i.p. injection at 10 μL/g of body weight | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05128734 | Not yet recruiting | Breast Cancer Triple Negative |
AHS Cancer Control Alberta |
July 1 2024 | Phase 2 |
| NCT05900895 | Not yet recruiting | Metastatic Breast Cancer |
Mary D Chamberlin|Dartmouth-Hitchcock Medical Center |
May 2024 | Phase 1 |
| NCT06377267 | Recruiting | Ovarian Cancer |
Vall d''Hebron Institute of Oncology |
February 6 2024 | Phase 2 |
| NCT06065059 | Recruiting | Breast Cancer|Ovarian Cancer|Pancreas Cancer|Prostate Cancer|BRCA1 Mutation|BRCA-Mutated Ovarian Carcinoma|BRCA-Associated Breast Carcinoma|HRD Positive Advanced Ovarian Cancer |
Tango Therapeutics Inc. |
December 8 2023 | Phase 1|Phase 2 |
Chemical Information & Solubility
| Molecular Weight | 434.46 | Formula | C24H23FN4O3 |
| CAS No. | 763113-22-0 | SDF | Download Olaparib (AZD2281) SDF |
| Smiles | C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F | ||
| Storage (From the date of receipt) | |||
|
In vitro |
DMSO : 87 mg/mL ( (200.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.) Water : Insoluble Ethanol : Insoluble |
Molecular Weight Calculator |
|
In vivo Add solvents to the product individually and in order. |
In vivo Formulation Calculator |
||||
Preparing Stock Solutions
Molarity Calculator
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
mg/kg
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
* Indicates a Required Field
Tags: buy Olaparib (AZD2281) | Olaparib (AZD2281) supplier | purchase Olaparib (AZD2281) | Olaparib (AZD2281) cost | Olaparib (AZD2281) manufacturer | order Olaparib (AZD2281) | Olaparib (AZD2281) distributor
Products are for research use only. Not for human use. We do not sell to patients.
©Copyright 2013 Selleck Chemicals. All Rights Reserved.