Olaparib (AZD2281)

别名: Ku-0059436 中文名称：奥拉帕尼

目录号：S1060 Purity: 99.99%

Olaparib (AZD2281, KU0059436)是选择性的PARP1/2抑制剂，IC50为5 nM/1 nM，其对PARP1/2的作用比对Tankyrase-1效果高300倍。在BRCA突变的细胞中，Olaparib可以显著地诱导线粒体自噬相关的细胞自噬。

Olaparib (AZD2281) Chemical Structure

CAS: 763113-22-0

规格	价格	库存
10mM (1mL in DMSO)	745.41	现货
10mg	794.43	现货
25mg	1219.52	现货
100mg	3019.32	现货
1g	7944.3	现货
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产品质控

批次：纯度： 99.99%

99.99

常与Olaparib (AZD2281)一起在实验中被使用的化合物

Niraparib (MK-4827)

在KMCH-1细胞中，Niraparib诱导凋亡并抑制抗凋亡蛋白的表达，而Olaparib对KMCH-1细胞诱导凋亡的影响最小。

Talazoparib (BMN 673)

Olaparib和Talazoparib被批准用于BRCA突变和HER2阴性乳腺癌患者的单药治疗。

Veliparib (ABT-888)

Olaparib显著抑制BRCA1和BRCA2突变细胞系的细胞存活，而Velaparib不诱导这些细胞系的细胞死亡。

Rucaparib

Olaparib和Rucaparib能有效阻断聚ADP核糖的形成，并在诱导HeLa细胞中PARP1捕获方面表现出相似的能力。

Paclitaxel

Olaparib和Paclitaxel联合Carboplatin可增强卵巢癌患者的疾病控制，降低复发率，且无额外毒副作用。

Olaparib (AZD2281)相关产品

相关靶点	PARP1 PARP2 PARP3 Tankyrase-1 Tankyrase-2 PARP14 PARP7 TNKS1 TNKS2	点击展开
相关产品	XAV-939 Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) A-966492 G007-LK UPF 1069 AZD2461 Pamiparib 3-Aminobenzamide ME0328 NMS-P118 Stenoparib (E7449) NVP-TNKS656 WIKI4 Benzamide NU1025 BGP-15 2HCl Picolinamide BYK204165 Fluzoparib (SHR-3162)	点击展开
相关化合物库	FDA药物库天然产物库凋亡分子化合物库 DNA损伤/ DNA修复化合物库细胞周期化合物库	点击展开

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息(PMID)
SGC-7901	Growth Inhibition Assay	30 μM	48 h	Block oxaliplatin-induced cell death	25767076
Huh7	Function Assay	40 μM	24 h	Induces cell autophagy with DHMEQ	25072752
Hep3B	Function Assay	40 μM	24 h	Induces cell autophagy with DHMEQ	25072752
Huh7	Function Assay	40 μM	24 h	Induces ROS production with DHMEQ	25072752
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	Significantly inhibits cell survival	20124459
Granta-519	Cytotoxic Assay	5 μM	96 h	Slightly inhibits cell survival	20124459
BT	Cytotoxic Assay	5 μM	96 h	Slightly inhibits cell survival	20124459
UPN2	Cytotoxic Assay	5 μM	96 h	Slightly inhibits cell survival	20124459
HBL-2	Cytotoxic Assay	5 μM	96 h	Slightly inhibits cell survival	20124459
JVM-2	Cytotoxic Assay	5 μM	96 h	Slightly inhibits cell survival	20124459
Z138	Cytotoxic Assay	5 μM	96 h	Slightly inhibits cell survival	20124459
RWPE	Invasive Assay	25 μM	48 h	Significantly reduces ERG-driven cell invasion	21575865
VCaP	Invasive Assay	25 μM	48 h	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
HCT116	Growth Inhibition Assay	100 μM	48 h	IC50=2.5 μM	24577941
SW1116	Growth Inhibition Assay	100 μM	48 h	IC50=100 μM	24577941
HT29	Growth Inhibition Assay	100 μM	48 h	IC50=14.7 μM	24577941
LoVo	Growth Inhibition Assay	100 μM	48 h	IC50=13.4 μM	24577941
HCT-15	Growth Inhibition Assay	100 μM	48 h	IC50=10 μM	24577941
SW48	Growth Inhibition Assay	100 μM	48 h	IC50=9.5 μM	24577941
C-1	Growth Inhibition Assay	100 μM	48 h	IC50=7.6 μM	24577941
RKO	Growth Inhibition Assay	100 μM	48 h	IC50=5.9 μM	24577941
HCT116	Growth Inhibition Assay	100 μM	48 h	Potentiates SN-38 cytotoxicity	24577941
SW1116	Growth Inhibition Assay	100 μM	48 h	Potentiates SN-38 cytotoxicity	24577941
HT29	Growth Inhibition Assay	100 μM	48 h	Potentiates SN-38 cytotoxicity	24577941
LoVo	Growth Inhibition Assay	100 μM	48 h	Potentiates SN-38 cytotoxicity	24577941
SW48	Growth Inhibition Assay	100 μM	48 h	Potentiates SN-38 cytotoxicity	24577941
C-1	Growth Inhibition Assay	100 μM	48 h	Potentiates SN-38 cytotoxicity	24577941
RKO	Growth Inhibition Assay	100 μM	48 h	Potentiates SN-38 cytotoxicity	24577941
HCT116	Function Assay	10 nM	12 h	Increases DNA double-strand breaks induced by SN-38	24577941
HT29	Function Assay	10 nM	12 h	Increases DNA double-strand breaks induced by SN-38	24577941
TE-6	Function Assay	5 μM	12 h	Induces G2/M arrest	24219164
TE-6	Function Assay	5 μM	24 h	Increases in double strand breaks (DSBs)	24219164
Hep3B	Growth Inhibition Assay	40 μM	72 h	Synergistically inhibits cell growth with DHMEQ	25072752
Huh7	Growth Inhibition Assay	40 μM	72 h	Synergistically inhibits cell growth with DHMEQ	25072752
Hep3B	Function Assay	40 μM	24 h	Induces ROS production with DHMEQ	25072752
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
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
Sf9	streptavidin-horseradish peroxidase-based luminescence assay			IC50=1.8 μM	29856625
Sf9	streptavidin-horseradish peroxidase-based luminescence assay			IC50=1.7 μM	26546219
Sf9	streptavidin-horseradish peroxidase-based luminescence assay			IC50=1.2 μM	29856625
A2780	SRB assay			IC50=1 μM	24398383
VC8	CCK8 or SRB assay			IC50=0.5656 μM	28692916
VC8	Cytotoxicity assay			CC50=0.468 μM	24815508
VC8	CCK8 assay			CC50=0.456 μM	29335205
Capan1	CCK8 or SRB assay			IC50=0.3993 μM	28692916
Capan1	Cytotoxicity assay			EC50=0.259 μM	26652717
LoVo	Celltiter-Glo assay			GI50=0.237 μM	26652717
VC8	Cytotoxicity assay			CC50=0.201 μM	23473053
UWB1.289	cell-titer glo assay			EC50=0.2 μM	29856625
Jurkat	MTS assay in presence of 100 uM of temozolomide			EC50=0.06 μM	23850199
MDA-MB-436	Cytotoxicity assay			CC50=0.0432 μM	23473053
MDA-MB-436	CCK8 or SRB assay			IC50=0.0393 μM	28692916
MX1	Cytotoxicity assay			EC50=0.0232 μM	26652717
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
MDA-MB-436	Cytotoxicity assay			CC50=0.0169 μM	24815508
OVCAR8	Binding affinity to PARP1			IC50=0.006 μM	29856625
SW620	Ex vivo inhibition of PARP1			IC50=0.006 μM	18800822
Sf9	UV/Vis spectrophotometric analysis			IC50=0.00359 μM	28601509
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	streptavidin-horseradish peroxidase-based luminescence assay			IC50=0.003 μM	26546219
Sf9	UV/Vis spectrophotometric analysis			IC50=0.00281 μM	28601509
HeLa	fluorescence assay			EC50=0.0025 μM	24398383
G7	immunofluorescence assay			IC50=0.0016 μM	26469301
T98G	immunofluorescence assay			IC50=0.0016 μM	26469301
Sf9	streptavidin-horseradish peroxidase-based luminescence assay			IC50=0.001 μM	26546219
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
点击查看更多细胞系数据

生物活性

产品描述

特性

Olaparib是第一批PARP抑制剂之一。

靶点

PARP2 ^[1] (Cell-free assay)	PARP1 ^[1] (Cell-free assay)
1 nM	5 nM

体外研究(In Vitro)
体外研究活性	Olaparib是PARP抑制剂，也作用于BRCA1或BRCA2突变。Olaparib对端锚(聚合)酶-1作用效果不大，IC50值大于1 μM。Olaparib浓度为30-100 nM作用于SW620细胞，使PARP-1失活。与BRCA1和BRCA2充足细胞系(Hs578T,MDA-MB-231,T47D)相比，BRCA1缺陷细胞系(MDA-MB-463和HCC1937)对Olaparib过分敏感^[1] Olaparib抑制PARP，阻断碱基切除修复，导致KB2P细胞对Olaparib强烈敏感。结果导致在DNA复制时由单链断裂转变为双链断裂，由此激活BRCA2依赖的重组途径。^[2]
激酶实验	体外独立酶实验
激酶实验	通过PARP-1实验测定PARP-2抑制活性，实验在96孔板上进行，PARP-2特定抗体与重组PARP-2蛋白结合。加入³H-NAD⁺DNA测定PARP-2活性。冲洗后，加入闪烁剂测定³H-渗透的核糖基化。通过AlphaScreen实验测定端锚聚合酶-1, 实验中HIS标签重组TANK-1蛋白和生物素化的NAD⁺ 在384孔Proxi板上温育。加入Alpha 磁珠，与HIS和生物素化的标签结合，产生邻近信号，测定信号消失的比例来计算TANK-1抑制活性。
细胞实验	细胞系	胸腺癌细胞系SW620结肠, A2780卵巢,HCC1937,Hs578T,MDA-MB-231,MDA-MB-436,和T47D
	浓度	1到300 nM
	孵育时间	7-14天
	方法	通过成株实验测定Olaparib毒性。Olaparib溶于DMSO中，用培养基稀释。细胞接种在六孔板上，过夜使粘附。然后加入不同浓度Olaparib，温育7-14天。计算存活菌落，测定IC50值。
实验图片	检测方法	检测指标	实验图片	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

体内研究(In Vivo)
体内研究活性	Olaparib有效作用于Brca1^-/-;p53^-/- 乳腺肿瘤 (每天按50 mg/kg剂量腹腔注射),但是对 HR缺陷的Ecad^-/-;p53^-/-乳腺肿瘤没有效果。Olaparib作用于携带肿瘤的鼠没有剂量限制毒性。^[3] Olaparib已经用于治疗BRCA突变的肿瘤, 比如卵巢癌，胸腺癌，前列腺癌。此外，Olaparib抑制ATM缺陷的肿瘤细胞具有选择性，说明Olaparib可作为治疗ATM突变的淋巴肿瘤的潜在试剂。^[4]
动物实验	Animal Models	携带Brca1^-/-;p53^-/-乳腺癌的 K14cre;Brca1^F/F;p53^F/F鼠
	Dosages	50 mg/kg
	Administration	按10 μL/g剂量腹腔注射

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考文献
https://pubmed.ncbi.nlm.nih.gov/18800822/ https://pubmed.ncbi.nlm.nih.gov/18559613/ https://pubmed.ncbi.nlm.nih.gov/18971340/ https://pubmed.ncbi.nlm.nih.gov/20739657/ + 展开

参考文献

https://pubmed.ncbi.nlm.nih.gov/18800822/
https://pubmed.ncbi.nlm.nih.gov/18559613/
https://pubmed.ncbi.nlm.nih.gov/18971340/

https://pubmed.ncbi.nlm.nih.gov/20739657/

+ 展开

化学信息&溶解度

分子量	434.46	分子式	C₂₄H₂₃FN₄O₃
CAS号	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
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 125 mg/mL ( (287.71 mM) Warmed with 50°C water bath; Ultrasonicated; ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 87 mg/mL ( (200.24 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 43 mg/mL ( (98.97 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 86 mg/mL ( (197.94 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂				动物体内配方计算器
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	9.000mg/ml (20.72mM)	以 1 mL 工作液为例，取100μL90mg/ml的澄清DMSO储备液加到400μL PEG300中，混合均匀使其澄清；向上述体系中加入50μLTween80，混合均匀使其澄清；然后继续加入450μL ddH2O定容至 1 mL。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	10%DMSO 1 90%Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	10.000mg/ml (23.02mM)	以 1 mL 工作液为例，取100μL100mg/ml的澄清DMSO储备液加到900μL玉米油中，混合均匀。工作液请现配现用！
澄清溶液	10% DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	11.000mg/ml (25.32mM)	以 1 mL 工作液为例,取100 μL 110mg/ml的澄清DMSO储备液加到400 μL PEG300中,混合均匀使其澄清;向上述体系中加入50 μL Tween80,混合均匀使其澄清;然后继续加入450 μL ddH2O定容至1mL。工作液请现配现用!
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	7.500mg/ml (17.26mM)	以 1 mL 工作液为例,取50μL150mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

* 必填项

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Olaparib (AZD2281)

产品质控

常与Olaparib (AZD2281)一起在实验中被使用的化合物

Olaparib (AZD2281)相关产品

相关信号通路图

细胞实验数据示例

生物活性

化学信息&溶解度

实验计算

技术支持