Olaparib

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Description: Potent PARP inhibitor
Chemical Name: 4-[[3-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinone
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

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.

Select a batch to recalculate based on the batch molecular weight:
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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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

Citations for Olaparib

Citations are publications that use Tocris products.

Currently there are no citations for Olaparib. Do you know of a great paper that uses Olaparib from Tocris? Please let us know.

Reviews for Olaparib

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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