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AZD2281 (Olaparib) PARP inhibitor

Name: AZD2281 (Olaparib)
Brand: Selleck Chemicals
SKU: S1060
Rating: 5 (1286 reviews)

N. Cat.: 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.

AZD2281 (Olaparib) PARP inhibitor Chemical Structure

Struttura chimica

Peso molecolare: 434.46

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.99%

99.99

Prodotti spesso usati con 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.

Target correlati	HDAC ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase eIF
Altro PARP Inibitori	XAV-939 AZD5305 (Saruparib) PJ34 HCl AG-14361 Iniparib (BSI-201) G007-LK A-966492 UPF 1069 Pamiparib ME0328

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Formulazione	Descrizione dell'attività	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
Clicca per visualizzare più dati sperimentali sulle linee cellulari

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	434.46	Formula	C₂₄H₂₃FN₄O₃	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	763113-22-0	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	Ku-0059436			Smiles	C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 125 mg/mL (287.71 mM) Riscaldato con bagno d'acqua a 60°C; Sonicato;
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Caratteristiche	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) agirebbe contro le mutazioni BRCA1 o BRCA2 e non è sensibile alla tankyrase-1 (IC50 >1 μM). Potrebbe annullare l'attività di PARP-1 a concentrazioni di 30-100 nM nelle cellule SW620. Questo composto è ipersensibile alle linee cellulari deficienti in BRCA1 (MDA-MB-463 e HCC1937), rispetto alle linee cellulari competenti in BRCA1 e BRCA2 (Hs578T, MDA-MB-231 e T47D). È fortemente sensibile alle cellule KB2P a causa della soppressione della riparazione per escissione di base da parte dell'inibizione di PARP, che può comportare la conversione di rotture a singolo filamento in rotture a doppio filamento durante la replicazione del DNA, attivando così le vie di ricombinazione dipendenti da BRCA2.
Saggio chinasico	Saggio FlashPlate (saggio di screening a 96 pozzetti)
Saggio chinasico	Nelle colonne da 1 a 10, viene aggiunto 1 μL di Olaparib (AZD2281) (in DMSO), e solo 1 μL di DMSO viene aggiunto ai pozzetti di controllo positivo (POS) e negativo (NEG) (rispettivamente colonne 11 e 12) di una FlashPlate pretrattata. PARP-1 viene diluita 1:40 in tampone (tampone B: 10% glicerolo (v/v), 25 mM HEPES, 12,5 mM MgCl₂, 50 mM KCl, 1 mM DTT, 0,01% NP-40 (v/v), pH 7,6) e 40 μL vengono aggiunti a tutti i 96 pozzetti (la concentrazione finale di PARP-1 nel saggio è di circa 1 ng/μL). La piastra viene sigillata e agitata a temperatura ambiente per 15 min. Successivamente, 10 μL di miscela di reazione positiva (0,2 ng/μL di oligonucleotidi a doppio filamento [M3/M4] DNA per pozzetto, 5 μM di concentrazione finale di NAD⁺ nel saggio e 0,075 μCi di ³H-NAD⁺ per pozzetto) vengono aggiunti ai pozzetti appropriati (colonne 1-11). La miscela di reazione negativa, priva dell'oligonucleotide DNA, viene aggiunta alla colonna 12 (con il valore medio del controllo negativo utilizzato come background). La piastra viene nuovamente sigillata e agitata per altri 60 min a temperatura ambiente per consentire alla reazione di continuare. Quindi, 50 μL di acido acetico ghiacciato (30%) vengono aggiunti a ciascun pozzetto per arrestare la reazione, e la piastra viene sigillata e agitata per altri 60 min a temperatura ambiente. Il segnale tritiato legato alla FlashPlate viene quindi determinato in conteggi per minuto (CPM) utilizzando il lettore di piastre TopCount.
In vivo	Olaparib (AZD2281) (10 mg/kg, p.o.) in combinazione sopprime significativamente la crescita tumorale negli xenotrapianti SW620. Mostra un'ottima risposta ai tumori mammari Brca1^-/-;p53^-/- (50 mg/kg i.p. al giorno), mentre nessuna risposta ai tumori mammari Ecad^-/-;p53^-/- deficienti in HR. Questo composto non mostra nemmeno tossicità dose-limitante nei topi portatori di tumore. È stato utilizzato per trattare tumori con mutazioni BRCA, come i tumori ovarici, mammari e prostatici. Inoltre, mostra un'inibizione selettiva delle cellule tumorali deficienti in ATM (Ataxia Telangiectasia Mutated), il che indica che potrebbe essere un potenziale agente per il trattamento dei tumori linfoidi mutanti ATM.
Riferimenti	[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/

Applicazioni (Applications)

Metodi	Biomarcatori	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

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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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