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Submit ReviewOlaparib
Description: Potent PARP inhibitor
Chemical Name: 4-[[3-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinone
Purity: ≥98% (HPLC)
Biological Activity for Olaparib
Olaparib is a potent PARP2 and PARP1 inhibitor (IC50 values are 1 and 5 nM, respectively). Olaparib abolishes PARP-1 activity at a concentration of 30-100 nM in SW620 cell lysates. BRCA1-deficient cell lines are hypersensitive to PARP inhibition by Olaparib in comparison with BRCA1- and BRCA2-proficient cells. Olaparib potentiates the antitumor activity of the methylating chemotherapeutic agent Temozolomide (Cat. No. 2706) in xenograft mouse model. Olaparib is orally bioavailable in rats.
Technical Data for Olaparib
| M. Wt | 434.47 |
| Formula | C24H23FN4O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 763113-22-0 |
| PubChem ID | 23725625 |
| InChI Key | FDLYAMZZIXQODN-UHFFFAOYSA-N |
| Smiles | O=C1NN=C(C=2C=CC=CC12)CC3=CC=C(F)C(=C3)C(=O)N4CCN(C(=O)C5CC5)CC4 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Olaparib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 2.17 | 5 with gentle warming | |
| DMSO | 43.45 | 100 |
Preparing Stock Solutions for Olaparib
The following data is based on the product molecular weight 434.47. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.3 mL | 11.51 mL | 23.02 mL |
| 5 mM | 0.46 mL | 2.3 mL | 4.6 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets for Olaparib
References for Olaparib
References are publications that support the biological activity of the product.
Menear et al (2008) 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. 51 6581 PMID: 18800822
Raimundo et al (2021) BBIT20 inhibits homologous DNA repair with disruption of the BRCA1-BARD1 interaction in breast and ovarian cancer. Br.J.Pharmacol. 178 3627 PMID: 33899955
If you know of a relevant reference for Olaparib, please let us know.
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Keywords: Olaparib, Olaparib supplier, potent, PARP1, PARP2, inhibitor, orally, bioavailable, BRCA1deficient, cell, antitumor, activity, Poly(ADP-ribose), Polymerase, 7579, Tocris Bioscience
1 Citation for Olaparib
Citations are publications that use Tocris products. Selected citations for Olaparib include:
Monika et al (2022) Sequential Targeting of PLK1 and PARP1 Reverses the Resistance to PARP Inhibitors and Enhances Platin-Based Chemotherapy in BRCA-Deficient High-Grade Serous Ovarian Cancer with KRAS Amplification. Int J Mol Sci 23 PMID: 36142803
Do you know of a great paper that uses Olaparib from Tocris? Please let us know.
Reviews for Olaparib
Average Rating: 5 (Based on 1 Review.)
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Filter by:
PARP inhibitor.
By
Kishor Pant on 11/30/2022
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: RBE and HepG2
It's an excellent selective inhibitor of PARP. This drug induces DNA damage in cancer cells. Used at 1-10 uM.
Literature in this Area
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Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.