Olaparib (Synonyms: 奥拉帕尼; AZD2281; KU0059436)

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摩尔计算器

Olaparib (AZD2281; KU0059436) 是一种口服有效的 PARP 抑制剂，抑制 PARP-1 和 PARP-2 的 IC₅₀ 分别为 5 和 1 nM。Olaparib 是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 激活剂。

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Olaparib Chemical Structure

CAS No. : 763113-22-0

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥567	In-stock
5 mg	￥321	In-stock
10 mg	￥515	In-stock
25 mg	￥880	In-stock
50 mg	￥1300	In-stock
100 mg	￥1980	In-stock
200 mg	￥2950	In-stock
500 mg	￥4950	In-stock
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Customer Review

Other Forms of Olaparib:

Olaparib-d₅ In-stock
Olaparib-d₈ In-stock
Olaparib-d₄-1 In-stock
Olaparib (Standard) In-stock

MCE 顾客使用本产品发表的 211 篇科研文献

Proliferation Assay

IHC

: Olaparib purchased from MCE. Usage Cited in: EBioMedicine. 2019 May;43:225-237. [Abstract]; Representative images of immunohistochemical staining for proteins as indicated in A2780 xenografted tumors (n=6 per treatment group) treated with Olaparib and PD 0332991 either as single-agents or in combination for 4 days.

: Olaparib purchased from MCE. Usage Cited in: EBioMedicine. 2019 Jun;44:419-430. [Abstract]; Immunoblots (IB) are done to detect γH2AX and DNA repair proteins, Ku80 and RAD51 using UAB-PA4 or UAB-PA16 tumors harvested from mice 24 h following final treatment. Quantitation by densitometry of results is shown below each IB image.

: Olaparib purchased from MCE. Usage Cited in: J Biomed Sci. 2019 Feb 4;26(1):14. [Abstract]; Inhibition of NFBD1 results in defective γ-H2AX foci formation after Olaparib exposure, cells are exposed to Olaparib for 24 h, and the γ-H2AX positive cells are determined by FCM

: Olaparib purchased from MCE. Usage Cited in: Mol Cancer Res. 2019 Jan;17(1):42-53. [Abstract]; Combination of RAD001 with Olaparib (left panel) and AZD2014 with Olaparib (right panel) activates the RIPK1 Ser 166 phosphorylation in Clone A and SF-539 cells respectively.

: Olaparib purchased from MCE. Usage Cited in: Gynecol Oncol. 2019 Jan;152(1):157-165. [Abstract]; Immunohistochemistry of RAD51 and γ-H2AX in samples of SKOV3 tumors. Representative sections are taken from tumor tissue of control, scrambled shRNA treated, Olaparib + scrambled shRNA treated, or Olaparib + CCND1-shRNA treated mice.

: Olaparib purchased from MCE. Usage Cited in: Gynecol Oncol. 2019 Jan;152(1):157-165. [Abstract]; Immunohistochemistry for CCND1 is performed in tumor samples in the treatment of compounds (control, scrambled shRNA treated, Olaparib + scrambled shRNA treated, or Olaparib + CCND1-shRNA treated).

: Olaparib purchased from MCE. Usage Cited in: Gynecol Oncol. 2019 Jan;152(1):157-165. [Abstract]; CCDN1 protein level in tumor samples of different treatment groups (control, scrambled shRNA treated, Olaparib + scrambled shRNA treated, or Olaparib + CCND1-shRNA treated) are analyzed by western blot.

: Olaparib purchased from MCE. Usage Cited in: Gynecol Oncol. 2019 Jan;152(1):157-165. [Abstract]; The expression of CCND1mRNA and cyclin D1 protein level in A2780 and SKOV3 cells is analyzed by western blot after Olaparib treatment at IC₅₀ concentrations.

: Olaparib purchased from MCE. Usage Cited in: Oncogene. 2018 Jan 18;37(3):341-351. [Abstract]; PTEN-deficient endometrioid endometrial cancer cell lines are treated with drugs as indicated for 24 h. Phosphorylated AKT, S6RP and 4EBP1 proteins and cleaved PARP are detected by western blot. Vinculin served as a loading control.

: Olaparib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2018 Dec;17(12):2676-2688. [Abstract]; EW8 and TC71 cells are treated with Olaparib (5 μM) or U0126 (5 μM) for 24 hours and then protein synthesis is assessed using puromycin labeling.

: Olaparib purchased from MCE. Usage Cited in: Oncol Rep. 2018 Apr;39(4):1747-1756. [Abstract]; The effect of Olaparib on protein expression. Western blot assays of MUS81 and MCM2 expression levels in A2780 and SKOV3 cells after treatment with 5 μM Olaparib compared with a blank control.

: Olaparib purchased from MCE. Usage Cited in: Cancer Chemother Pharmacol. 2017 Oct;80(4):861-867. [Abstract]; PARP1 inhibition is lethal to MPM cells. Colony formation assays of clonal cell survival with continuous Niraparib or Olaparib, both at 3 uM. a H2452 BPA1-mutant MPM cells exposed to Niraparib. b HMeso01A BAP1-mutant MPM cells exposed to Niraparib. cHMeso01A BAP1-mutant MPM cells exposed to Olaparib. d CRL-2081 BAP1 wild-type MPM cells exposed to Olaparib. e CRL-2081 BAP1 wild-type MPM cells exposed to Niraparib. f Dose response of H2452 BPA1-mutant MPM cells exposed to varying concentrations of

: Olaparib purchased from MCE. Usage Cited in: Int J Mol Sci. 2016 Feb 24;17(3):272. [Abstract]; The effect of AZD2281 on the protein expression of xenografted HSC-2 tumors. Relative band intensity of western blot data is normalized by the expression level of β-actin; The proteins analyzed are PARP-1 (poly(ADP-ribose) polymerase-1).

Olaparib 相关产品

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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

细胞效力
(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]

体外研究
(In Vitro)

Olaparib (AZD2281) 是 PARP-1 和 PARP-2 的个位数纳摩尔抑制剂，对 BRCA1 缺陷型乳腺癌细胞系显示出独立的活性。将 Olaparib 应用于 SW620 细胞裂解物，确定 PARP-1 抑制的 IC₅₀ 约为 6 nM，PARP-1 活性的总消融浓度为 30 100 nM^[1]。

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

体内研究
(In Vivo)

携带 SW620 异种移植肿瘤的动物用 Olaparib (10 mg/kg，口服，每天 1 次，共 5 天) 与 NSC 362856 (TMZ) (50 mg/kg，口服) 联合处理抗肿瘤^[1]。Olaparib 增加在 DWC 模型中建立的 Calu-6 肿瘤的血管灌注。Olaparib (50 mg/kg，口服) 作为单一药物或与放疗联合使用导致 Calu-6 肿瘤的荧光强度增加^[2]。

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

Clinical Trial

分子量

434.46

Formula

C₂₄H₂₃FN₄O₃

CAS 号

763113-22-0

性状

固体

颜色

White to yellow

中文名称

奥拉帕尼；奥拉帕利

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (230.17 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

DMF 中的溶解度 : 50 mg/mL (115.09 mM; 超声助溶)

Ethanol 中的溶解度 : 3.12 mg/mL (7.18 mM; 超声助溶 (<60°C))

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 10 mg/mL (23.02 mM); 悬浊液; 超声助溶

此方案可获得 10 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 5 mg/mL (11.51 mM); 澄清溶液
方案三

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.51 mM); 澄清溶液
方案四

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.75 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案五

请依序添加每种溶剂： 10% DMF 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.75 mM); 澄清溶液
方案六

请依序添加每种溶剂： 10% DMF 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.75 mM); 澄清溶液
方案七

请依序添加每种溶剂： 10% DMF 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.75 mM); 澄清溶液
方案八

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.79 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案九

请依序添加每种溶剂： 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.15 mM); 澄清溶液

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 20 mg/mL (46.03 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.98%

选择批次：

Data Sheet (650 KB) SDS (393 KB)

COA (288 KB) HNMR (221 KB) LCMS (120 KB) 元素分析报告 (211 KB)

产品使用指南 (1538 KB)

参考文献

[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.
参考文献	[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]

Olaparib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Olaparib (Synonyms: 奥拉帕尼; AZD2281; KU0059436)

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Olaparib (Synonyms: 奥拉帕尼; AZD2281; KU0059436)

Customer Review

Other Forms of Olaparib:

Olaparib 相关抗体

MCE 顾客使用本产品发表的 211 篇科研文献

Olaparib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PARP 亚型特异性产品:

生物活性

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参考文献

Olaparib 相关抗体:

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