Home DNA Damage/DNA Repair PARP inhibitor - Mitophagy activator - Autophagy activator Olaparib (AZD2281) For research use only.

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

Olaparib (AZD2281) Chemical Structure

CAS: 763113-22-0

Selleck's Olaparib (AZD2281) has been cited by 1106 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Products often used together with Olaparib (AZD2281)

Niraparib (MK-4827)

Niraparib induces apoptosis and suppresses anti-apoptotic protein expression in KMCH-1 cells, while Olaparib has minimal impact on apoptosis induction in KMCH-1 cells.

Bezrookove V, et al. Cancers (Basel). 2021 Aug 31;13(17):4405.

Talazoparib (BMN 673)

Olaparib and Talazoparib are approved monotherapies for individuals with deleterious or suspected deleterious germline BRCA mutations and HER2-negative breast cancer.

Cortesi L, et al. Target Oncol. 2021 May;16(3):255-282.

Veliparib (ABT-888)

Olaparib significantly inhibits cell survival in BRCA1 and BRCA2 mutant cell lines, while Velaparib does not induce cell death in these cell lines.

Arun B, et al. Int J Oncol. 2015 Jul;47(1):262-8.

Rucaparib

Olaparib and Rucaparib potently block the formation of poly-ADP-ribose (PAR) and demonstrate approximately similar capabilities in inducing PARP1 trapping in HeLa cells.

Kim C, et al. Elife. 2020 Aug 26;9:e60637.

Paclitaxel

Olaparib and Paclitaxel combined with carboplatin enhance disease control and reduce the recurrence rate without extra toxic side effects in patients with ovarian cancer.

Zhang H, et al. Am J Transl Res. 2022 Jan 15;14(1):468-475. eCollection 2022.

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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
PARP2 [1]
(Cell-free assay)		 PARP1 [1]
(Cell-free assay)
1 nM 5 nM
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 Combining with temozolomide, Olaparib (10 mg/kg, p.o.) significantly suppresses tumor growth in SW620 xenografts. [1] Olaparib shows great response to Brca1-/-;p53-/- mammary tumors (50 mg/kg i.p. per day), while no responses to HR-deficient Ecad-/-;p53-/- mammary tumors. Olaparib even does not show dose-limiting toxicity in tumor-bearing mice. [3] Olaparib has been used to treat with BRCA mutated tumors, such as ovarian, breast and prostate cancers. Moreover, Olaparib shows selectively inhibition to ATM (Ataxia Telangiectasia Mutated)-deficient tumor cells, which indicates to be a potential agent for treating ATM mutant lymphoid tumors. [4]
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
NCT05900895 Not yet recruiting Metastatic Breast Cancer Dickinson|Dartmouth-Hitchcock Medical Center December 2023 Phase 1
NCT06065059 Recruiting Breast Cancer|Ovarian Cancer|Pancreas Cancer|Prostate Cancer|BRCA1 Mutation|BRCA-Mutated Ovarian Carcinoma|BRCA-Associated Breast Carcinoma|HRD Positive Advanced Ovarian Cancer Tango Therapeutics Inc. December 8 2023 Phase 1|Phase 2
NCT05128734 Not yet recruiting Breast Cancer Triple Negative AHS Cancer Control Alberta December 1 2023 Phase 2
NCT05887609 Recruiting Ovary Cancer|Peritoneal Cancer|Fallopian Tube Cancer University of Colorado Denver|ImmunoGen Inc. October 3 2023 Phase 2

Chemical lnformation & 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
Batch:

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
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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Frequently Asked Questions

Question 1:
How to prepare the solution of the compound (S1060) for in vivo study?

Answer:
We recommend the following formulation: 4% DMSO+30% PEG300+ 66%H2O. It is a clear solution and can be used for IP injection.

Question 2:
I saw that the solubility of the compound for in vivo on the website had been changed, why the change has been made?

Answer:
For the formulation for in vivo, the compound dissolving in 15% Captisol (former solubility) is a suspension, and it is fine for oral gavage. And now, dissolving in 4% DMSO+30% PEG 300+ddH2O is a clear solution, and is for injection.

Question 3:
How long can the chemical compound be stable in DMEM at 4 °C?

Answer:
The compound is stable in DMEM at 4 degree for one week.

PARP Signaling Pathway Map

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