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Olaparib

(CAS No:763113-22-0)
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.
CAS No:763113-22-0
Molecular Weight(MW):434.46
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 763113-22-0
Molecular formula(MF) C24H23FN4O3
Molecular Weight(MW): 434.46
Alias 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine
Solubility
In vitro DMSO 86 mg/mL warmed (197.94 mM)
Water 0.002 mg/mL (0.0 mM)
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+ddH2O 5mg/mL
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.
Features A potent PARP inhibitor (currently in late stage clinical trials).
Targets
PARP2 [1]
(Cell-free assay)
PARP1 [1]
(Cell-free assay)
Tankyrase-1 [1]
(Cell-free assay)
1 nM 5 nM 1.5 μM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KP3.33 Growth Inhibition Assay 4 d IC50=5.705 μM 18559613
KP6.3 Growth Inhibition Assay 4 d IC50=10.428 μM 18559613
KP7.7 Growth Inhibition Assay 4 d IC50=57 nM 18559613
KB2P3.4 Growth Inhibition Assay 4 d IC50=124 M 18559613
KB2P1.21 Growth Inhibition Assay 4 d IC50=8907 nM 18559613
U373-MG Cytotoxic Assay 1 μM 24 h Increases radiation sensitivity 18954712
T98G Cytotoxic Assay 1 μM 24 h Increases radiation sensitivity 18954712
U87-MG Cytotoxic Assay 1 μM 24 h Increases radiation sensitivity 18954712
UVW Cytotoxic Assay 500 nM 24 h Increases radiation sensitivity 18954712
HeLa Function Assay 500 nM 4 h Causes a modest delay in rejoining of radiation-induced DNA breaks 18954712
HeLa Function Assay 1 μM 24 h Enhances radiation-induced S-phase arrest 18954712
T98G Function Assay 1 μM 24 h Enhances radiation-induced S-phase arrest 18954712
L3 Cytotoxic Assay 5 μM 96 h DMSO Significantly inhibits cell survival 20124459
Granta-519 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
UPN2 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
JVM-2 Cytotoxic Assay 5 μM 96 h DMSO Slightly inhibits cell survival 20124459
Z138 Cytotoxic Assay 5 μM 96 h DMSO Slightly inhibits cell survival 20124459
RWPE Invasive Assay 25 μM 48 h DMSO Significantly reduces ERG-driven cell invasion 21575865
VCaP Invasive Assay 25 μM 48 h DMSO Significantly reduces ERG-driven cell invasion 21575865
Mouse H2AX−/− ES Cells Cytotoxic Assay 2.5 μM 20 h Significantly inhibits cell survival 23355489
Mouse ATM−/− ES Cells Cytotoxic Assay 2.5 μM 20 h Significantly inhibits cell survival 23355489
H1650 Growth Inhibition Assay 20 μM 144 h IC50=15.47 μM 23239809
H1650PTEN+ Growth Inhibition Assay 20 μM 144 h IC50=50.83 μM 23239809
PC-9 Growth Inhibition Assay 20 μM 144 h IC50=5.88 μM 23239809
PC-9PTEN− Growth Inhibition Assay 20 μM 144 h IC50=6.52 μM 23239809
MDA-MB-231 Growth Inhibition Assay 5 day IC50=6.9 μM 23760496
MDA-MB-468 Growth Inhibition Assay 5 day IC50=5.0 μM 23760496
BT20 Growth Inhibition Assay 5 day IC50=7.7 μM 23760496
HCC1143 Growth Inhibition Assay 5 day IC50=11.1 μM 23760496
HCC1937 Growth Inhibition Assay 5 day IC50=12.6 μM 23760496
Hs578t Growth Inhibition Assay 5 day IC50=5.6 μM 23760496
Hs578t(si) Growth Inhibition Assay 5 day IC50=7.5 μM 23760496
BT474 Growth Inhibition Assay 5 day IC50=19.8 μM 23760496
JIMT1 Growth Inhibition Assay 5 day IC50=7.7 μM 23760496
SKBR3 Growth Inhibition Assay 5 day IC50=11.1 μM 23760496
SUM159 Growth Inhibition Assay 5 day IC50=4.2 μM 23760496
CAMA1 Growth Inhibition Assay 5 day IC50=15.8 μM 23760496
MCF7 Growth Inhibition Assay 5 day IC50=5.8 μM 23760496
T47D Growth Inhibition Assay 5 day IC50=9.6 μM 23760496
HCT116 Growth Inhibition Assay 100 μM 48 h DMSO IC50=2.5 μM 24577941
SW1116 Growth Inhibition Assay 100 μM 48 h DMSO IC50=100 μM 24577941
HT29 Growth Inhibition Assay 100 μM 48 h DMSO IC50=14.7 μM 24577941
LoVo Growth Inhibition Assay 100 μM 48 h DMSO IC50=13.4 μM 24577941
HCT-15 Growth Inhibition Assay 100 μM 48 h DMSO IC50=10 μM 24577941
SW48 Growth Inhibition Assay 100 μM 48 h DMSO IC50=9.5 μM 24577941
C-1 Growth Inhibition Assay 100 μM 48 h DMSO IC50=7.6 μM 24577941
RKO Growth Inhibition Assay 100 μM 48 h DMSO IC50=5.9 μM 24577941
HCT116 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
HT29 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
SW48 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
RKO Growth Inhibition Assay 100 μM 48 h DMSO Potentiates SN-38 cytotoxicity 24577941
HCT116 Function Assay 10 nM 12 h DMSO Increases DNA double-strand breaks induced by SN-38 24577941
HT29 Function Assay 10 nM 12 h DMSO Increases DNA double-strand breaks induced by SN-38 24577941
TE-6 Function Assay 5 μM 12 h DMSO Induces G2/M arrest 24219164
TE-6 Function Assay 5 μM 24 h DMSO Increases in double strand breaks (DSBs) 24219164
Hep3B Growth Inhibition Assay 40 μM 72 h DMSO Synergistically inhibits cell growth with DHMEQ 25072752
Huh7 Growth Inhibition Assay 40 μM 72 h DMSO Synergistically inhibits cell growth with DHMEQ 25072752
Hep3B Function Assay 40 μM 24 h DMSO Induces ROS production with DHMEQ 25072752
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
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

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]