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AZD2281 (Olaparib) PARP inhibitor

Name: AZD2281 (Olaparib)
Brand: Selleck Chemicals
SKU: S1060
Rating: 5 (1281 reviews)

Cat.No.S1060

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.

Chemical Structure

Molecular Weight: 434.46

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Quality Control

Batch: Purity: 99.99%

99.99

Products Often Used Together with AZD2281 (Olaparib)

Veliparib (ABT-888)

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

Related Targets	HDAC ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase eIF
Other PARP Inhibitors	XAV-939 AZD5305 (Saruparib) PJ34 HCl AG-14361 Iniparib (BSI-201) G007-LK Pamiparib UPF 1069 A-966492 Stenoparib (E7449)

Cell Culture, Treatment & Working Concentration

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
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Chemical Information, Storage & Stability

Molecular Weight	434.46	Formula	C₂₄H₂₃FN₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	763113-22-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Ku-0059436			Smiles	C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F

Solubility

In vitro
Batch:

DMSO : 125 mg/mL (287.71 mM) Warmed with 50°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	9.000mg/ml (20.72mM)	Taking the 1 mL working solution as an example, add 100 μL of 90 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10%DMSO 1 90%Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (23.02mM)	Taking the 1 mL working solution as an example, add 100 μL of 100 mg/ml clear DMSO stock solution to 900 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	10% DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	11.000mg/ml (25.32mM)	Taking the 1 mL working solution as an example, add 100 μL of 110 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	7.500mg/ml (17.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Features	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) would act against BRCA1 or BRCA2 mutations and is not sensitive to tankyrase-1 (IC50 >1 μM). It could ablate the PARP-1 activity at concentrations of 30-100 nM in SW620 cells. This compound 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). It 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.
Kinase Assay	FlashPlate assay (96-well screening assay)
Kinase Assay	To columns 1 through 10, 1 μL of Olaparib (AZD2281) (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.
In vivo	Olaparib (AZD2281) (10 mg/kg, p.o.) in Combination significantly suppresses tumour growth in SW620 xenografts. It shows great response to Brca1^-/-;p53^-/- mammary tumours (50 mg/kg i.p. per day), while no responses to HR-deficient Ecad^-/-;p53^-/- mammary tumours. This compound even does not show dose-limiting toxicity in tumour-bearing mice. It has been used to treat with BRCA mutated tumours, such as ovarian, breast and prostate cancers. Moreover, it shows selectively inhibition to ATM (Ataxia Telangiectasia Mutated)-deficient tumour cells, which indicates to be a potential agent for treating ATM mutant lymphoid tumours.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18800822/ [2] https://pubmed.ncbi.nlm.nih.gov/18559613/ [3] https://pubmed.ncbi.nlm.nih.gov/18971340/ [4] https://pubmed.ncbi.nlm.nih.gov/20739657/

Applications

Methods	Biomarkers	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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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