Olaparib (AZD2281)

别名: Ku-0059436 中文名称:奥拉帕尼

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

Olaparib (AZD2281) Chemical Structure

CAS: 763113-22-0

规格 价格 库存 购买数量
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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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。


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

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。


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

Veliparib (ABT-888)


Olaparib显著抑制BRCA1BRCA2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。


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

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。


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

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。


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

Olaparib (AZD2281)相关产品

相关信号通路图

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
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
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生物活性

产品描述 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。
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
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;Brca1F/F;p53F/F
Dosages 50 mg/kg
Administration 按10 μL/g剂量腹腔注射
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

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)

体外溶解度
批次:

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

摩尔浓度计算器

体内溶解度
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

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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,: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: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: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。

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