主页 / 药理学 / Enzymes / Polymerases / Poly(ADP-ribose) Polymerase / Poly(ADP-Ribose) Polymerase Inhibitors / Olaparib

Olaparib

Cat. No. 7579 1 次引用 1 条评论 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
Pricing Availability   Qty
说明： Potent PARP inhibitor
化学名： 4-[[3-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinone
纯度： ≥98% (HPLC)
说明书
引用文献 (1)
评论 (1)
文献 (2)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 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.

技术数据 for Olaparib

分子量 434.47
公式 C24H23FN4O3
储存 Store at -20°C
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Olaparib

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
ethanol 2.17 5 温和加热
DMSO 43.45 100

制备储备液 for Olaparib

以下数据基于产品分子量 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

参考文献 for Olaparib

参考文献是支持产品生物活性的出版物。

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.

按标靶查看相关产品

按产品操作查看相关产品

查看全部 Poly(ADP-Ribose) Polymerase Inhibitors

关键词: Olaparib, Olaparib supplier, potent, PARP1, PARP2, inhibitor, orally, bioavailable, BRCA1deficient, cell, antitumor, activity, Poly(ADP-ribose), Polymerase, 7579, Tocris Bioscience

1 篇 Olaparib 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Olaparib 的部分引用包括：

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

您是否知道使用了 Tocris Olaparib 的优秀论文？ 请告知我们.

Olaparib 的评论

平均评分: 5 (Based on 1 Review.)

5 星
100%
4 星
0%
3 星
0%
2 星
0%
1 星
0%

Have you used Olaparib?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Filter by:


PARP inhibitor.
By Kishor Pant on 11/30/2022
分析类型： In Vitro
种属： Human
细胞系/组织： RBE and HepG2

It's an excellent selective inhibitor of PARP. This drug induces DNA damage in cancer cells. Used at 1-10 uM.

review image

该领域的文献

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

*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。

Cell Cycle and DNA Damage Research Product Guide

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

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.