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Olaparib (AZD2281)

Catalog No.: A10111

PARP inhibitor

Olaparib (AZD2281)

Olaparib (AZD2281) Chemical Structure

CAS NO. 763113-22-0

Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.

Availability: In stock

Package Price Qty
10 mg

Regular Price: $40.00

Special Price $32.00

25 mg

Regular Price: $60.00

Special Price $48.00

50 mg

Regular Price: $70.00

Special Price $56.00

100 mg

Regular Price: $90.00

Special Price $72.00

10mM * 1mL in DMSO

Regular Price: $76.00

Special Price $60.80

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  • Saptarshi Sinha, .et al. Olaparib enhances the Resveratrol-mediated apoptosis in breast cancer cells by inhibiting the homologous recombination repair pathway, Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
  • Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
  • Yuki Uchihara, .et al. DNA damage promotes HLA class I presentation by stimulating a pioneer round of translation-associated antigen production, Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
  • Ji-Ye Kim, .et al. ARL6IP5 reduces cisplatin-resistance by suppressing DNA repair and promoting apoptosis pathways in ovarian carcinoma, Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
  • Emad Matanes, .et al. Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents, Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
  • Shino Endo, .et al. BRCA1/ATF1-Mediated Transactivation is Involved in Resistance to PARP Inhibitors and Cisplatin, Cancer Res Commun, 2021, 1(2): 90-105
  • Yan Baglo, .et al. Evolutionary dynamics of cancer multidrug resistance in response to olaparib and photodynamic therapy, Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
  • Joseph M Gozgit, .et al. PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity, Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
  • Sefinew Molla, .et al. Olaparib enhances curcumin-mediated apoptosis in oral cancer cells by inducing PARP trapping through modulation of BER and chromatin assembly, DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
  • Jianming Wang, .et al. Persistence of RNA transcription during DNA replication delays duplication of transcription start sites until G2/M, Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
  • Ai Ito, .et al. Metolazone upregulates mitochondrial chaperones and extends lifespan in Caenorhabditis elegans, Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
  • Tim J Wigle, .et al. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement, Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
  • Ali Divan, .et al. Structurally unique PARP-1 inhibitors for the treatment of prostate cancer, Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
  • Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
  • Sai Dimple Manavitha Gullipalli, .et al. Development and Validation of Bioanalytical Method for Estimation of Niraparib in Rat Plasma Using High Performance LC-MS/MS And Its Application to Pharmacokinetic Study, Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
  • Chao Zhang, .et al. Phenotypic Switching of Atherosclerotic Smooth Muscle Cells is Regulated by Activated PARP1-Dependent TET1 Expression, J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
  • Wigle TJ, .et al. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes, SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
  • Wang Q, .et al. Biguanides in combination with olaparib limits tumorigenesis of drug-resistant ovarian cancer cells through inhibition of Snail, Cancer Med, 2019, Dec 21 PMID: 31863638
  • Molla S, .et al. PARP inhibitor Olaparib Enhances the Apoptotic Potentiality of Curcumin by Increasing the DNA Damage in Oral Cancer Cells through Inhibition of BER Cascade, Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
  • Alvin Z.Lu, .et al. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation, Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
  • Bian C, .et al. NADP+ is an endogenous PARP inhibitor in DNA damage response and tumor suppression, Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
  • HC de Silva, .et al. IGFBP-3 interacts with NONO and SFPQ in PARP-dependent DNA damage repair in triple-negative breast cancer, Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
  • Kamada Y, .et al. Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II, Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
  • 2018, .et al. Augmentation of the therapeutic efficacy of WEE1 kinase inhibitor AZD1775 by inhibiting the YAP-E2F1-DNA damage response pathway axis, FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
  • Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
  • Hiro Sato, .et al. DNA double-strand break repair pathway regulates PD-L1 expression in cancer cells, Nat Commun, 2017, 8: 1751 PMID: 29170499
  • Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
  • Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189

Biological Activity

Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.
Targets
PARP2 (Cell-free assay) PARP1 (Cell-free assay) Tankyrase-1 (Cell-free assay)
1 nM5 nM1.5 μM
In vitro (25°C) DMSO Warmed: 74 mg/mL (170.32 mM)
Water <1 mg/mL
Ethanol Insoluble
In vivo 4% DMSO+30% PEG 300+ddH2O 4 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 23.01 mL 115.07 mL 230.15 mL
0.5 mM 4.6 mL 23.01 mL 46.03 mL
1 mM 2.3 mL 11.51 mL 23.01 mL
5 mM 0.46 mL 2.3 mL 4.6 mL

*The above data is based on the productmolecular weight 434.5 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Catalog Num A10111
Actions Inhibitor
CAS No. 763113-22-0
Formula C24H23FN4O3
M. Wt 434.5
Purity >98%
Synonyms KU-0059436
SMILES C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F
Storage

Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for 36 months.
In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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