HY-10162-1ml | Olaparib [763113-22-0] Clinisciences

Description

Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC₅₀s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator^[1]^[2]^[3]^[4].

IC₅₀ & Target^[1]

PARP-2

1 nM (IC₅₀)

PARP-1

5 nM (IC₅₀)

tankyrase-1

1.5 μM (IC₅₀)

Autophagy

Mitophagy

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	1 μM Compound: Olaparib, KU-59436, AZD 2281	Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay	[PMID: 24398383]
A549	IC₅₀	28 μM Compound: 1, AZD2281, KU0059436	In vitro antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay In vitro antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24521039]
AML12	CC₅₀	31.09 μM Compound: Olaparib	Cytotoxicity against mouse AML12 cells assessed as reduction in cell viability incubated for 7 days by MTT assay Cytotoxicity against mouse AML12 cells assessed as reduction in cell viability incubated for 7 days by MTT assay	[PMID: 35504210]
Bel-7402	IC₅₀	35.5 μM Compound: Olaparib	Antiproliferative activity against human Bel-7402 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human Bel-7402 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 30844273]
Caco-2	IC₅₀	65.5 μM Compound: Olaparib	Antiproliferative activity against human Caco-2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human Caco-2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 30844273]
CAPAN-1	IC₅₀	0.027 μM Compound: 5; OLA	Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 13 days by by CCK-8 assay Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 13 days by by CCK-8 assay	[PMID: 32924477]
CAPAN-1	IC₅₀	0.053 μM Compound: OL	Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 5 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 5 days by MTT assay	[PMID: 35780655]
CAPAN-1	IC₅₀	0.053 μM Compound: Olaparib	Antiproliferative activity against human BRCA2 -/- CAPAN-1 cells assessed as reduction in cell viability incubated for 5 to 10 days by MTT assay Antiproliferative activity against human BRCA2 -/- CAPAN-1 cells assessed as reduction in cell viability incubated for 5 to 10 days by MTT assay	[PMID: 35430559]
CAPAN-1	IC₅₀	0.53 μM Compound: 1; AZD2281	Antiproliferative activity against BRCA2-deficient human CAPAN-1 cells assessed as inhibition of cell proliferation incubated for 7 days by CellTiter-Glo assay Antiproliferative activity against BRCA2-deficient human CAPAN-1 cells assessed as inhibition of cell proliferation incubated for 7 days by CellTiter-Glo assay	[PMID: 35785724]
CAPAN-1	IC₅₀	2.61 μM Compound: Olaparib	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
CAPAN-1	IC₅₀	25.2 μM Compound: Olaparib	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay	[PMID: 35091172]
CAPAN-1	IC₅₀	399.3 nM Compound: 1; AZD-2281	Antiproliferative activity against human Capan1 cells after 7 days by CCK8 or SRB assay Antiproliferative activity against human Capan1 cells after 7 days by CCK8 or SRB assay	[PMID: 28692916]
CAPAN-1	IC₅₀	5.34 μM Compound: Olaparib	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay	[PMID: 35091172]
CAPAN-1	IC₅₀	6.3 μM Compound: Olaparib, KU-59436, AZD 2281	Antiproliferative activity against BRCA2 gene mutated human Capan1 cells after 72 hrs by SRB assay Antiproliferative activity against BRCA2 gene mutated human Capan1 cells after 72 hrs by SRB assay	[PMID: 24398383]
CAPAN-1	IC₅₀	8.42 μM Compound: Olaparib	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay	[PMID: 35091172]
CAPAN-1	IC₅₀	8.42 μM Compound: Olaparib	Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability after 4 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 34813314]
CAPAN-1	IC₅₀	83.1 μM Compound: Ola	Antiproliferative activity against BRCA2-deficient human Capan1 cells after 48 hrs by MTT assay Antiproliferative activity against BRCA2-deficient human Capan1 cells after 48 hrs by MTT assay	[PMID: 32222339]
CFPAC-1	IC₅₀	13.7 μM Compound: Olaparib	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay	[PMID: 35091172]
CFPAC-1	IC₅₀	13.7 μM Compound: Olaparib	Antiproliferative activity against human CFPAC-1 cells assessed as reduction in cell viability after 4 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 34813314]
CFPAC-1	IC₅₀	28.7 μM Compound: Olaparib	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay	[PMID: 35091172]
CFPAC-1	IC₅₀	7.44 μM Compound: Olaparib	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
CFPAC-1	IC₅₀	9.87 μM Compound: Olaparib	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay	[PMID: 35091172]
CWR22R	IC₅₀	33.8 μM Compound: Olaparib	Growth inhibition of human 22Rv1 cells after 5 days by SRB assay Growth inhibition of human 22Rv1 cells after 5 days by SRB assay	[PMID: 32484346]
DLD-1	IC₅₀	0.042 μM Compound: 1	Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days	[PMID: 34570508]
DLD-1	EC₅₀	0.1 μM Compound: 2	Antiproliferative activity against BRCA deficient human DLD1 cells by Celltiter-Glo assay Antiproliferative activity against BRCA deficient human DLD1 cells by Celltiter-Glo assay	[PMID: 31303996]
DLD-1	EC₅₀	19 μM Compound: 2	Antiproliferative activity against human DLD1 cells by Celltiter-Glo assay Antiproliferative activity against human DLD1 cells by Celltiter-Glo assay	[PMID: 31303996]
DU-145	IC₅₀	17.7 μM Compound: Olaparib	Growth inhibition of human DU145 cells after 5 days by SRB assay Growth inhibition of human DU145 cells after 5 days by SRB assay	[PMID: 32484346]
ES-2	IC₅₀	2.05 μM Compound: Olaparib	Antiproliferative activity against human ES2 cells assessed as reduction in cell viability measured after 7 days Antiproliferative activity against human ES2 cells assessed as reduction in cell viability measured after 7 days	[PMID: 35643262]
HCC1937	IC₅₀	> 10 μM Compound: Olaparib	Antiproliferative activity against human BRCA-1 deficient HCC1937 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay Antiproliferative activity against human BRCA-1 deficient HCC1937 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay	[PMID: 33740547]
HCC1937	IC₅₀	> 200 μM Compound: ola	Cytotoxicity against human HCC1937 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human HCC1937 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35393219]
HCC1937	IC₅₀	> 200 μM Compound: Ola	Antiproliferative activity against BRCA1-deficient human HCC1937 cells after 48 hrs by MTT assay Antiproliferative activity against BRCA1-deficient human HCC1937 cells after 48 hrs by MTT assay	[PMID: 32222339]
HCC1937	IC₅₀	10.3 μM Compound: Olaparib, KU-59436, AZD 2281	Antiproliferative activity against BRCA1 gene mutated human HCC1937 cells after 72 hrs by SRB assay Antiproliferative activity against BRCA1 gene mutated human HCC1937 cells after 72 hrs by SRB assay	[PMID: 24398383]
HCC1937	IC₅₀	4.97 μM Compound: Olaparib	Antiproliferative activity against human HCC1937 cells harboring BRCA1 mutant after 72 hrs by MTT assay Antiproliferative activity against human HCC1937 cells harboring BRCA1 mutant after 72 hrs by MTT assay	[PMID: 28763648]
HCC1937	IC₅₀	8.65 μM Compound: Olaparib	Antiproliferative activity against human HCC1937 cells after 3 days by MTT assay Antiproliferative activity against human HCC1937 cells after 3 days by MTT assay	[PMID: 28601509]
HCC1937	IC₅₀	83.1 μM Compound: Olaparib	Antiproliferative activity against BRCA deficient human HCC1937 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against BRCA deficient human HCC1937 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 34998039]
HCC827	IC₅₀	> 50 μM Compound: Olaparib	Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay	[PMID: 28601509]
HCT-116	IC₅₀	> 10 μM Compound: Olaparib	Antiproliferative activity against human BRCA-2 deficient HCT-116 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay Antiproliferative activity against human BRCA-2 deficient HCT-116 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay	[PMID: 33740547]
HCT-116	IC₅₀	15.13 μM Compound: Olaparib	Antiproliferative activity against human HCT116 cells expressing topoisomerase-1 after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells expressing topoisomerase-1 after 72 hrs by MTT assay	[PMID: 28763648]
HCT-116	IC₅₀	5.56 μM Compound: Olaparib	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 7 days by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 7 days by MTT assay	[PMID: 35504210]
HCT-116	IC₅₀	7.32 μM Compound: Olaparib	Antiproliferative activity against BRCA2-mutated human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against BRCA2-mutated human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
HeLa	IC₅₀	> 50 μM Compound: Olaparib	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 28601509]
HeLa	EC₅₀	2.5 nM Compound: Olaparib, KU-59436, AZD 2281	Inhibition of PARP-1 in human HeLa cells assessed as decrease of H2O2-induced PARylation after 3 hrs by fluorescence assay Inhibition of PARP-1 in human HeLa cells assessed as decrease of H2O2-induced PARylation after 3 hrs by fluorescence assay	[PMID: 24398383]
HepG2	IC₅₀	42.4 μM Compound: Olaparib	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 30844273]
Jurkat	EC₅₀	0.06 μM Compound: AZD-2281	Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomide Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomide	[PMID: 23850199]
Jurkat	EC₅₀	16 μM Compound: AZD-2281	Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay	[PMID: 23850199]
K562	IC₅₀	> 50 μM Compound: Olaparib	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay Antiproliferative activity against human K562 cells after 72 hrs by MTT assay	[PMID: 28601509]
L02	IC₅₀	25.8 μM Compound: Olaparib	Cytotoxicity against human HL7702 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Cytotoxicity against human HL7702 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 30844273]
LoVo	GI₅₀	237 nM Compound: 2; AZD-2281	Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay	[PMID: 26652717]
LoVo	EC₅₀	3.57 nM Compound: 2; AZD-2281	Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay	[PMID: 26652717]
MCF-10A	IC₅₀	> 1000 μM Compound: Olaparib	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 24 hrs by Hoechst 33342/propidium iodide staining based fluorescence analysis Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 24 hrs by Hoechst 33342/propidium iodide staining based fluorescence analysis	[PMID: 36603398]
MCF-10A	IC₅₀	> 1000 μM Compound: Olaparib	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by Hoechst 33342/propidium iodide staining based fluorescence analysis Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by Hoechst 33342/propidium iodide staining based fluorescence analysis	[PMID: 36603398]
MCF-10A	IC₅₀	> 50 μM Compound: Olaparib	Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay	[PMID: 28601509]
MCF7	IC₅₀	< 1000 μM Compound: Olaparib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by Hoechst 33342/propidium iodide staining based fluorescence analysis Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by Hoechst 33342/propidium iodide staining based fluorescence analysis	[PMID: 36603398]
MCF7	IC₅₀	> 1000 μM Compound: Olaparib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 24 hrs by Hoechst 33342/propidium iodide staining based fluorescence analysis Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 24 hrs by Hoechst 33342/propidium iodide staining based fluorescence analysis	[PMID: 36603398]
MCF7	IC₅₀	> 200 μM Compound: Ola	Antiproliferative activity against BRCA-proficient human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against BRCA-proficient human MCF7 cells after 48 hrs by MTT assay	[PMID: 32222339]
MCF7	IC₅₀	> 40 μM Compound: Olaparib	Antiproliferative activity against human MCF7 cells incubated for 2 to 5 days by MTT assay Antiproliferative activity against human MCF7 cells incubated for 2 to 5 days by MTT assay	[PMID: 31153806]
MCF7	GI₅₀	13.2 μM Compound: Olaparib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition by MTT assay	[PMID: 32088129]
MCF7	IC₅₀	232 μM Compound: Olaparib	Antiproliferative activity against BRCA proficient human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against BRCA proficient human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 34998039]
MCF7	IC₅₀	35.24 μM Compound: Olaparib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 28601509]
MCF7	IC₅₀	36.24 μM Compound: Olaparib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 28763648]
MCF7	IC₅₀	409.1 μM Compound: ola	Cytotoxicity against human MCF7 cells harbouring wild type BRCA1/2 assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human MCF7 cells harbouring wild type BRCA1/2 assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35393219]
MDA-MB-231	IC₅₀	< 1000 μM Compound: Olaparib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by Hoechst 33342/propidium iodide staining based fluorescence analysis Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by Hoechst 33342/propidium iodide staining based fluorescence analysis	[PMID: 36603398]
MDA-MB-231	IC₅₀	> 10 μM Compound: Olaparib	Antiproliferative activity against human BRCA proficient MDA-MB-231 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay Antiproliferative activity against human BRCA proficient MDA-MB-231 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay	[PMID: 33740547]
MDA-MB-231	IC₅₀	> 200 μM Compound: ola	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35393219]
MDA-MB-231	IC₅₀	> 200 μM Compound: Ola	Antiproliferative activity against BRCA-proficient human MDA-MB-231 cells after 48 hrs by MTT assay Antiproliferative activity against BRCA-proficient human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 32222339]
MDA-MB-231	IC₅₀	> 40 μM Compound: Olaparib	Antiproliferative activity against human MDA-MB-231 cells incubated for 2 to 5 days by MTT assay Antiproliferative activity against human MDA-MB-231 cells incubated for 2 to 5 days by MTT assay	[PMID: 31153806]
MDA-MB-231	IC₅₀	0.69 μM Compound: Olaparib	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 7 days Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 7 days	[PMID: 35643262]
MDA-MB-231	IC₅₀	32.36 μM Compound: Olaparib	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 96 hrs by CCK8 assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 96 hrs by CCK8 assay	[PMID: 32726747]
MDA-MB-231	IC₅₀	39.51 μM Compound: Olaparib	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 28601509]
MDA-MB-231	GI₅₀	4.23 μM Compound: Olaparib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition by MTT assay	[PMID: 32088129]
MDA-MB-231	IC₅₀	4.47 μM Compound: OL	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 5 days by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 5 days by MTT assay	[PMID: 35780655]
MDA-MB-231	IC₅₀	4.47 μM Compound: Olaparib	Antiproliferative activity against wild type human MDA-MB-231 cells assessed as reduction in cell viability incubated for 5 to 10 days by MTT assay Antiproliferative activity against wild type human MDA-MB-231 cells assessed as reduction in cell viability incubated for 5 to 10 days by MTT assay	[PMID: 35430559]
MDA-MB-231	IC₅₀	5.35 μM Compound: Olaparib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 7 days by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 7 days by MTT assay	[PMID: 35504210]
MDA-MB-231	IC₅₀	62.5 μM Compound: Olaparib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
MDA-MB-231	IC₅₀	7.92 μM Compound: Olaparib	Antiproliferative activity against human MDA-MB-231 cells after 5 days by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 5 days by MTT assay	[PMID: 28601509]
MDA-MB-231	IC₅₀	8.48 μM Compound: Olaparib	Antiproliferative activity against BRCA-proficient human MDA-MB-231 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against BRCA-proficient human MDA-MB-231 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
MDA-MB-231	IC₅₀	8.48 μM Compound: Olaparib	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 7 days Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 7 days	[PMID: 34813314]
MDA-MB-436	CC₅₀	0.0169 μM Compound: AZD2281	Cytotoxicity against BRCA1-deficient human MDA-MB-436 cells by sulforhodamine B assay Cytotoxicity against BRCA1-deficient human MDA-MB-436 cells by sulforhodamine B assay	[PMID: 24815508]
MDA-MB-436	IC₅₀	0.018 μM Compound: 5; OLA	Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 7 days by CCK-8 assay Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 7 days by CCK-8 assay	[PMID: 32924477]
MDA-MB-436	IC₅₀	0.02 μM Compound: OL	Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 5 days by MTT assay Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 5 days by MTT assay	[PMID: 35780655]
MDA-MB-436	IC₅₀	0.02 μM Compound: Olaparib	Antiproliferative activity against human BRCA1 -/- MDA-MB-436 cells assessed as reduction in cell viability incubated for 5 to 10 days by MTT assay Antiproliferative activity against human BRCA1 -/- MDA-MB-436 cells assessed as reduction in cell viability incubated for 5 to 10 days by MTT assay	[PMID: 35430559]
MDA-MB-436	IC₅₀	0.1 μM Compound: 1; AZD2281	Antiproliferative activity against BRCA1-deficient human MDA-MB-436 cells assessed as inhibition of cell proliferation incubated for 7 days by CCK-8 assay Antiproliferative activity against BRCA1-deficient human MDA-MB-436 cells assessed as inhibition of cell proliferation incubated for 7 days by CCK-8 assay	[PMID: 35785724]
MDA-MB-436	IC₅₀	0.22 μM Compound: Olaparib	Antiproliferative activity against human MDA-MB-436 cells harboring BRCA1 mutation incubated for 2 to 5 days by MTT assay Antiproliferative activity against human MDA-MB-436 cells harboring BRCA1 mutation incubated for 2 to 5 days by MTT assay	[PMID: 31153806]
MDA-MB-436	IC₅₀	39.3 nM Compound: 1; AZD-2281	Antiproliferative activity against human MDA-MB-436 cells after 7 days by CCK8 or SRB assay Antiproliferative activity against human MDA-MB-436 cells after 7 days by CCK8 or SRB assay	[PMID: 28692916]
MDA-MB-468	IC₅₀	> 10 μM Compound: Olaparib	Antiproliferative activity against human BRCA proficient MDA-MB-468 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay Antiproliferative activity against human BRCA proficient MDA-MB-468 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay	[PMID: 33740547]
MDA-MB-468	IC₅₀	1.83 μM Compound: Olaparib	Antiproliferative activity against BRCA-proficient human MDA-MB-468 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against BRCA-proficient human MDA-MB-468 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
MDA-MB-468	IC₅₀	10.1 μM Compound: Olaparib	Cytotoxicity against human MDA-MB-468 cells measured after 72 hrs by Celltiter-Glo assay Cytotoxicity against human MDA-MB-468 cells measured after 72 hrs by Celltiter-Glo assay	[PMID: 33200929]
MDA-MB-468	IC₅₀	13.72 μM Compound: Olaparib	Antiproliferative activity against human MDA-MB-468 cells measured after 7 days by Celltiter-glo assay Antiproliferative activity against human MDA-MB-468 cells measured after 7 days by Celltiter-glo assay	[PMID: 33309164]
MDA-MB-468	IC₅₀	2.52 μM Compound: Olaparib	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 7 days by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 7 days by MTT assay	[PMID: 35504210]
MDA-MB-468	IC₅₀	200 μM Compound: ola	Cytotoxicity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35393219]
MDA-MB-468	IC₅₀	4.19 μM Compound: OL	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 5 days by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 5 days by MTT assay	[PMID: 35780655]
MDA-MB-468	IC₅₀	4.19 μM Compound: Olaparib	Antiproliferative activity against human PTEN -/- MDA-MB-468 cells assessed as reduction in cell viability incubated for 5 to 10 days by MTT assay Antiproliferative activity against human PTEN -/- MDA-MB-468 cells assessed as reduction in cell viability incubated for 5 to 10 days by MTT assay	[PMID: 35430559]
MEF	EC₅₀	14.6 μM Compound: AZD2281	Cytotoxicity against mouse wild type MEF cells assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay Cytotoxicity against mouse wild type MEF cells assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay	[PMID: 29856625]
MEF	EC₅₀	49.6 μM Compound: AZD2281	Cytotoxicity against mouse PARP1 deficient MEF cells assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay Cytotoxicity against mouse PARP1 deficient MEF cells assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay	[PMID: 29856625]
MEF	EC₅₀	8.5 μM Compound: AZD2281	Cytotoxicity against mouse PARP2 deficient MEF cells expressing PARP1 assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay Cytotoxicity against mouse PARP2 deficient MEF cells expressing PARP1 assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay	[PMID: 29856625]
MX1	IC₅₀	35.8 μM Compound: ola	Cytotoxicity against human MX1 cells harbouring BRCA1 mutant assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human MX1 cells harbouring BRCA1 mutant assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35393219]
MX1	IC₅₀	35.8 μM Compound: Ola	Antiproliferative activity against BRCA1-deficient human MX1 cells after 48 hrs by MTT assay Antiproliferative activity against BRCA1-deficient human MX1 cells after 48 hrs by MTT assay	[PMID: 32222339]
NCI-H1299	IC₅₀	35.93 μM Compound: Cpd P	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 34038131]
NCI-H1355	IC₅₀	33 μM Compound: 1, AZD2281, KU0059436	In vitro antiproliferative activity against human NCI-H1355 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay In vitro antiproliferative activity against human NCI-H1355 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24521039]
NCI-H1693	IC₅₀	19 μM Compound: 1, AZD2281, KU0059436	In vitro antiproliferative activity against human NCI-H1693 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay In vitro antiproliferative activity against human NCI-H1693 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24521039]
NCI-H1703	IC₅₀	20 μM Compound: 1, AZD2281, KU0059436	In vitro antiproliferative activity against human NCI-H1703 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay In vitro antiproliferative activity against human NCI-H1703 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24521039]
NCI-H1792	IC₅₀	16 μM Compound: 1, AZD2281, KU0059436	In vitro antiproliferative activity against human NCI-H1792 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay In vitro antiproliferative activity against human NCI-H1792 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24521039]
NCI-H1944	IC₅₀	25 μM Compound: 1, AZD2281, KU0059436	In vitro antiproliferative activity against human NCI-H1944 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay In vitro antiproliferative activity against human NCI-H1944 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24521039]
NCI-H2030	IC₅₀	34 μM Compound: 1, AZD2281, KU0059436	In vitro antiproliferative activity against human NCI-H2030 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay In vitro antiproliferative activity against human NCI-H2030 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24521039]
NCI-H2122	IC₅₀	38 μM Compound: 1, AZD2281, KU0059436	In vitro antiproliferative activity against human NCI-H2122 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay In vitro antiproliferative activity against human NCI-H2122 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24521039]
NCI-H23	IC₅₀	10 μM Compound: 1, AZD2281, KU0059436	In vitro antiproliferative activity against human H23 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay In vitro antiproliferative activity against human H23 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24521039]
NCI-H322M	IC₅₀	50 μM Compound: 1, AZD2281, KU0059436	In vitro antiproliferative activity against human NCI-H322M cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay In vitro antiproliferative activity against human NCI-H322M cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24521039]
NCI-H441	IC₅₀	28 μM Compound: 1, AZD2281, KU0059436	In vitro antiproliferative activity against human H441 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay In vitro antiproliferative activity against human H441 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24521039]
NCI-H460	IC₅₀	12 μM Compound: 1, AZD2281, KU0059436	In vitro antiproliferative activity against human H460 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay In vitro antiproliferative activity against human H460 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 24521039]
OCI-LY19	GI₅₀	0.849 μM Compound: Olaparib	Cytotoxicity against human OCI-LY19 assessed as growth inhibition after 3 days by Alamar Blue assay Cytotoxicity against human OCI-LY19 assessed as growth inhibition after 3 days by Alamar Blue assay	[PMID: 26546219]
PC-3	IC₅₀	20.6 μM Compound: Olaparib	Growth inhibition of human PC3 cells after 5 days by SRB assay Growth inhibition of human PC3 cells after 5 days by SRB assay	[PMID: 32484346]
Raji	IC₅₀	> 50 μM Compound: Olaparib	Antiproliferative activity against human Raji cells after 3 days by MTT assay Antiproliferative activity against human Raji cells after 3 days by MTT assay	[PMID: 28601509]
Sf9	IC₅₀	0.001 μM Compound: Olaparib	Inhibition of full length human PARP1 expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay Inhibition of full length human PARP1 expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay	[PMID: 26546219]
Sf9	IC₅₀	0.003 μM Compound: Olaparib	Inhibition of human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay Inhibition of human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay	[PMID: 26546219]
Sf9	IC₅₀	0.036 μM Compound: Olaparib	Inhibition of recombinant human full length C-terminal His-tagged PARP1 expressed in Sf9 insect cells preincubated for 15 mins followed by NAD+ addition and measured after 40 mins by fluorescence based assay Inhibition of recombinant human full length C-terminal His-tagged PARP1 expressed in Sf9 insect cells preincubated for 15 mins followed by NAD+ addition and measured after 40 mins by fluorescence based assay	[PMID: 31153806]
Sf9	IC₅₀	0.139 μM Compound: AZD-2281	Inhibition of N-terminal GST-tagged human PARP1 expressed in a Baculovirus infected Sf9 insect cells using biotinylated substrate incubated for 1 hr by colorimetric method Inhibition of N-terminal GST-tagged human PARP1 expressed in a Baculovirus infected Sf9 insect cells using biotinylated substrate incubated for 1 hr by colorimetric method	[PMID: 31401008]
Sf9	IC₅₀	0.5 nM Compound: Ola	Inhibition of human N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay Inhibition of human N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay	[PMID: 31042381]
Sf9	IC₅₀	1.2 nM Compound: Ola	Inhibition of human full-length N-terminal GST-tagged PARP1 expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay Inhibition of human full-length N-terminal GST-tagged PARP1 expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay	[PMID: 31042381]
Sf9	IC₅₀	1.7 μM Compound: Olaparib	Inhibition of human TNKS2 (667 to 1166 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay Inhibition of human TNKS2 (667 to 1166 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay	[PMID: 26546219]
Sf9	IC₅₀	1.8 nM Compound: Olaparib	Inhibition of recombinant human full length N-terminal GST- tagged PARP1 expressed in baculovirus infected sf9 cells using Colorimetric HRP as substrate incubated for 30 mins by UV/Vis spectrophotometer analysis Inhibition of recombinant human full length N-terminal GST- tagged PARP1 expressed in baculovirus infected sf9 cells using Colorimetric HRP as substrate incubated for 30 mins by UV/Vis spectrophotometer analysis	[PMID: 31442685]
Sf9	IC₅₀	1.8 μM Compound: Olaparib	Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay	[PMID: 26546219]
Sf9	IC₅₀	1.9 μM Compound: Olaparib	Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay	[PMID: 26546219]
SK-BR-3	IC₅₀	< 1000 μM Compound: Olaparib	Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell growth incubated for 72 hrs by Hoechst 33342/propidium iodide staining based fluorescence analysis Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell growth incubated for 72 hrs by Hoechst 33342/propidium iodide staining based fluorescence analysis	[PMID: 36603398]
SK-BR-3	IC₅₀	232 μM Compound: ola	Cytotoxicity against human SK-BR-3 cells harbouring wild type BRCA1/2 assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human SK-BR-3 cells harbouring wild type BRCA1/2 assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35393219]
SK-BR-3	IC₅₀	232 μM Compound: Ola	Antiproliferative activity against BRCA-proficient human SKBR3 cells after 48 hrs by MTT assay Antiproliferative activity against BRCA-proficient human SKBR3 cells after 48 hrs by MTT assay	[PMID: 32222339]
SK-OV-3	IC₅₀	1910 μM Compound: 3, AZD2281	Cytotoxicity against human SKOV3 cells after 7 days by sulforhodamine B assay Cytotoxicity against human SKOV3 cells after 7 days by sulforhodamine B assay	[PMID: 23473053]
SK-OV-3	IC₅₀	20.9 nM Compound: 3, AZD2281	Inhibition of PARP1/PARP2 in human SKOV3 cells assessed as reduction in H2O2-induced PARylation incubated for 4 hrs prior to H2O2 treatment Inhibition of PARP1/PARP2 in human SKOV3 cells assessed as reduction in H2O2-induced PARylation incubated for 4 hrs prior to H2O2 treatment	[PMID: 23473053]
SK-OV-3	IC₅₀	3.15 μM Compound: Olaparib	Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 30844273]
SUM149PT	EC₅₀	0.4 μM Compound: Ola	Cytotoxicity against BRCA1-deficient human SUM149 cells measured after 6 days by microscopic analysis Cytotoxicity against BRCA1-deficient human SUM149 cells measured after 6 days by microscopic analysis	[PMID: 31042381]
SUM149PT	EC₅₀	7 μM Compound: Ola	Cytotoxicity against BRCA1-proficient human SUM149 cells measured after 6 days by microscopic analysis Cytotoxicity against BRCA1-proficient human SUM149 cells measured after 6 days by microscopic analysis	[PMID: 31042381]
SW1990	IC₅₀	19.4 μM Compound: Olaparib	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth after 3 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth after 3 days by MTT assay	[PMID: 35091172]
SW1990	IC₅₀	3.63 μM Compound: Olaparib	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
SW1990	IC₅₀	4.93 μM Compound: Olaparib	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 5 days by MTT assay	[PMID: 35091172]
SW1990	IC₅₀	5.73 μM Compound: Olaparib	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 4 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 4 days by MTT assay	[PMID: 35091172]
SW1990	IC₅₀	5.73 μM Compound: Olaparib	Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability after 4 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 34813314]
SW-620	IC₅₀	> 10 μM Compound: Olaparib	Antiproliferative activity against human BRCA-2 proficient SW-620 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay Antiproliferative activity against human BRCA-2 proficient SW-620 cells assessed as reduction in cell growth incubated for 7 days by cell titer-glo assay	[PMID: 33740547]
SW-620	IC₅₀	6 nM Compound: 47, KU0059436, AZD-2281	Ex vivo inhibition of PARP1 in human SW620 cells assessed as amount of poly(ADP-ribose) by whole cell assay Ex vivo inhibition of PARP1 in human SW620 cells assessed as amount of poly(ADP-ribose) by whole cell assay	[PMID: 18800822]
T47D	IC₅₀	> 50 μM Compound: Olaparib	Antiproliferative activity against human T47D cells after 72 hrs by MTT assay Antiproliferative activity against human T47D cells after 72 hrs by MTT assay	[PMID: 28601509]
T98G	IC₅₀	1.6 nM Compound: 1	Inhibition of PARP1 in human T98G cells incubated for 60 mins by immunofluorescence assay Inhibition of PARP1 in human T98G cells incubated for 60 mins by immunofluorescence assay	[PMID: 26469301]
THP-1	IC₅₀	32.3 μM Compound: Olaparib	Antiproliferative activity against human THP-1 cells expressing BRD4 assessed as inhibition of cell growth measured after 3 days by MTT assay Antiproliferative activity against human THP-1 cells expressing BRD4 assessed as inhibition of cell growth measured after 3 days by MTT assay	[PMID: 35091172]
U-937	IC₅₀	21.81 μM Compound: Olaparib	Antiproliferative activity against human U937 cells after 72 hrs by MTT assay Antiproliferative activity against human U937 cells after 72 hrs by MTT assay	[PMID: 28601509]
V79	IC₅₀	≥ 10000 nM Compound: 1; AZD-2281	Cytotoxicity against BRCA2 expressing Chinese hamster V79 cells after 3 days by CCK8 or SRB assay Cytotoxicity against BRCA2 expressing Chinese hamster V79 cells after 3 days by CCK8 or SRB assay	[PMID: 28692916]
V79	CC₅₀	8.985 μM Compound: AZD2281	Cytotoxicity against Chinese hamster V79 cells by sulforhodamine B assay Cytotoxicity against Chinese hamster V79 cells by sulforhodamine B assay	[PMID: 24815508]

In Vitro

Olaparib (AZD2281) is a single digit nanomolar inhibitor of both PARP-1 and PARP-2 that shows standalone activity against BRCA1-deficient breast cancer cell lines. Olaparib is applied to SW620 cell lysates, and identified the IC₅₀ for PARP-1 inhibition to be around 6 nM and the total ablation of PARP-1 activity to be at concentrations of 30 100 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Animals bearing SW620 xenografted tumors are treated with Olaparib (10 mg/kg, p.o.) in combination with NSC 362856 (TMZ) (50 mg/kg, p.o.) once daily for 5 consecutive days, after which the tumors are left to grow out^[1]. Olaparib increases vascular perfusion in Calu-6 tumors established in a DWC model. Administration of olaparib(50 mg/kg, p.o.) as a single agent (top panel) or in combination with radiation (bottom panel) results in an increase in fluorescence intensity in the Calu-6 tumors^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

434.46

Formula

C₂₄H₂₃FN₄O₃

CAS No.

763113-22-0

Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=CC(CC(C2=C3C=CC=C2)=NNC3=O)=CC=C1F)N4CCN(C(C5CC5)=O)CC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (230.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : 50 mg/mL (115.09 mM; Need ultrasonic)

Ethanol : 3.12 mg/mL (7.18 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3017 mL	11.5085 mL	23.0171 mL
5 mM	0.4603 mL	2.3017 mL	4.6034 mL
10 mM	0.2302 mL	1.1509 mL	2.3017 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 10 mg/mL (23.02 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 10 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 5 mg/mL (11.51 mM); Clear solution
Protocol 3

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.51 mM); Clear solution
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 5

Add each solvent one by one: 10% DMF 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution
Protocol 6

Add each solvent one by one: 10% DMF 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution
Protocol 7

Add each solvent one by one: 10% DMF 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution
Protocol 8

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 9

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.15 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 20 mg/mL (46.03 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.98%

Select Batch:

SDS (393 KB)

COA (250 KB) HNMR (221 KB) LCMS (120 KB) Elemental Analysis Report (108 KB)

Handling Instructions (2659 KB)

References

[1]. Menear KA, et al. 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581-91 [Content Brief]

[2]. Senra JM, et al. Inhibition of PARP-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft.Mol Cancer Ther. 2011 Oct;10(10):1949-58. [Content Brief]

[3]. Yasukawa M, et al. Synergetic Effects of PARP Inhibitor AZD2281 in Oral Squamous Cell Carcinoma in Vitro and in Vivo. Int J Mol Sci. 2016 Feb 24;17(3):272. [Content Brief]

[4]. Bian X, et al. PTEN deficiency sensitizes endometrioid endometrial cancer to compound PARP-PI3K inhibition but not PARP inhibition as monotherapy. Oncogene. 2018 Jan 18;37(3):341-351. [Content Brief]

Kinase Assay ^[1]	This assay determined the ability of Olaparib to inhibit PARP-1 enzyme activity. PARP-2 activity inhibition is measured by using a variation of the PARP-1 assay in which PARP-2 protein (recombinant) is bound down by a PARP-2 specific antibody in a 96-well white-walled plate. PARP-2 activity is measured following ³H-NAD⁺ DNA additions. After washing, scintillant is added to measure ³H-incorporated ribosylations. For tankyrase-1, an AlphaScreen assay is developed in which HIS-tagged recombinant TANK-1 protein is incubated with biotinylated NAD⁺ in a 384-well ProxiPlate assay. Alpha beads are added to bind the HIS and biotin tags to create a proximity signal, whereas the inhibition of TANK-1 activity is directly proportional to the loss of this signal. All experiments are repeated at least three times^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	The PF₅₀ value is the potentiation factor, which is calculated as the ratio of the IC₅₀ of the control growth with alkylating agent methylmethane sulfonate (MMS) divided by the IC₅₀ of the MMS combined with the PARP inhibitor. HeLa B cells are used, and Olaparib is tested at a fixed 200 nM concentration for screening with MMS. For the testing of Olaparib on the SW620 colorectal cell line, the concentrations that are used are 1, 3, 10, 100 and 300 nM. Cell growth is assessed by the use of the sulforhodamine B (SRB) assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] Mice bearing 220-250 mm³ tumors are randomized into 4 treatment groups (n=5): A; vehicle control (10% DMSO in PBS/10% 2-hydroxy-propyl-β-cyclodextrin daily for 5 days by oral gavage), B; Olaparib (50 mg/kg daily for 5 days by oral gavage), C; 10 Gy fractionated radiotherapy (2 Gy daily for 5 days), D; Olaparib and 10 Gy (5×2 Gy) fractionated radiotherapy (with olaparib given 30 min prior to each daily 2 Gy dose of radiation). Tumor volume measurements are determined daily until they reached 1000 mm³. The number of days for each individual tumor to quadruple in size from the start of the treatment (relative tumor volume×4; RTV4) is calculated for the individual tumors in each group. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Menear KA, et al. 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581-91 [Content Brief] [2]. Senra JM, et al. Inhibition of PARP-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft.Mol Cancer Ther. 2011 Oct;10(10):1949-58. [Content Brief] [3]. Yasukawa M, et al. Synergetic Effects of PARP Inhibitor AZD2281 in Oral Squamous Cell Carcinoma in Vitro and in Vivo. Int J Mol Sci. 2016 Feb 24;17(3):272. [Content Brief] [4]. Bian X, et al. PTEN deficiency sensitizes endometrioid endometrial cancer to compound PARP-PI3K inhibition but not PARP inhibition as monotherapy. Oncogene. 2018 Jan 18;37(3):341-351. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

Ethanol / DMF / DMSO	1 mM	2.3017 mL	11.5085 mL	23.0171 mL	57.5427 mL
Ethanol / DMF / DMSO	5 mM	0.4603 mL	2.3017 mL	4.6034 mL	11.5085 mL
DMF / DMSO	10 mM	0.2302 mL	1.1509 mL	2.3017 mL	5.7543 mL
	15 mM	0.1534 mL	0.7672 mL	1.5345 mL	3.8362 mL
	20 mM	0.1151 mL	0.5754 mL	1.1509 mL	2.8771 mL
	25 mM	0.0921 mL	0.4603 mL	0.9207 mL	2.3017 mL
	30 mM	0.0767 mL	0.3836 mL	0.7672 mL	1.9181 mL
	40 mM	0.0575 mL	0.2877 mL	0.5754 mL	1.4386 mL
	50 mM	0.0460 mL	0.2302 mL	0.4603 mL	1.1509 mL
	60 mM	0.0384 mL	0.1918 mL	0.3836 mL	0.9590 mL
	80 mM	0.0288 mL	0.1439 mL	0.2877 mL	0.7193 mL
	100 mM	0.0230 mL	0.1151 mL	0.2302 mL	0.5754 mL

Olaparib Related Classifications

Cell Cycle/DNA Damage Epigenetics Autophagy
PARP Autophagy Mitophagy

Olaparib [763113-22-0]

Cat# HY-10162-1ml

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

Other Forms of Olaparib:

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Complete Stock Solution Preparation Table

Olaparib Related Classifications

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Olaparib [763113-22-0]

Cat# HY-10162-1ml

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

Other Forms of Olaparib:

View All PARP Isoform Specific Products:

Olaparib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Olaparib Related Classifications

Keywords:

You might also be interested by the following products: