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抑制剂/激动剂
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类器官培养添加剂
PARP
/ Olaparib/奥拉帕尼

Olaparib/奥拉帕尼 {[allProObj[0].p_purity_real_show]}

货号：A134565 同义名： AZD2281; KU0059436

Olaparib 是一种 PARP 抑制剂，对 PARP1 和 PARP2 具有高亲和力，IC50 值分别为 5 nM 和 1 nM。Olaparib 具有抗肿瘤作用，可用于 BRCA 突变相关癌症的研究。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Olaparib/奥拉帕尼 化学结构 CAS号：763113-22-0
Olaparib/奥拉帕尼 化学结构
CAS号：763113-22-0
Olaparib/奥拉帕尼 3D分子结构
CAS号：763113-22-0
Olaparib/奥拉帕尼 化学结构 CAS号：763113-22-0
Olaparib/奥拉帕尼 3D分子结构 CAS号：763113-22-0
规格 价格 会员价 库存 数量
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Olaparib/奥拉帕尼 纯度/质量文件 产品仅供科研

货号：A134565 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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产品名称 PARP ↓ PARP1 ↓ PARP2 ↓ PARP3 ↓ 其他靶点 纯度
PJ34 HCl ++

PARP, EC50: 20 nM

 		99%+
Rucaparib phosphate ++++

PARP, Ki: 1.4 nM

 		99%+
3-Aminobenzamide ++

PARP, IC50: <50 nM

 		98%
AZD-2461 ✔ 99%+
BGP-15 ✔ 99%+
NU1025 +

PARP, IC50: 400 nM

 		98%
Benzamide +

PARP, IC50: 3.3 μM

 		98%
Picolinamide +

PARP, IC50: 95 μM

 		98%
AG14361 +++

PARP1, Ki: <5 nM

 		98+%
Iniparib ✔ 98%
Talazoparib ++++

PARP1, IC50: 0.57 nM

 		99%+
NMS-P118 ++

PARP1, Kd: 0.009 μM

 		97%
UPF 1069 +

PARP1, IC50: 8.0 μM

 		++

PARP2, IC50: 0.3 μM

 		98%
A-966492 ++++

PARP1, EC50: 1 nM

PARP1, Ki: 1 nM

 		+++

PARP2, Ki: 1.5 nM

 		99%+
Veliparib ++

PARP1, Ki: 5.2 nM

 		+++

PARP2, Ki: 2.9 nM

 		98%
Niraparib tosylate +++

PARP1, IC50: 3.8 nM

 		+++

PARP2, IC50: 2.1 nM

 		99%+
Stenoparib ++++

PARP1, IC50: 1 nM

 		++++

PARP2, IC50: 1.2 nM

 		98%
Olaparib +++

PARP1, IC50: 5 nM

 		++++

PARP2, IC50: 1 nM

 		98%
Niraparib +++

PARP1, IC50: 3.8 nM

 		+++

PARP2, IC50: 2.1 nM

 		98%
ME0328 +

PARP1, IC50: 6.3 μM

 		+

PARP3, IC50: 0.89 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Olaparib/奥拉帕尼 生物活性

靶点

  • PARP1

    PARP1, IC50:5 nM

  • PARP2

    PARP2, IC50:1 nM
描述 PARP1, also called as Poly(ADP-ribose) polymerase, is involved in the signaling of DNA damage. It can recognize and bind DNA single or double-strand breaks . Thus it possesses various cellular function, including regulation of apoptosis and chromosome stability, gene amplification and transcription, as well as cell division and differentiation. PARP-2 is the closest homolog of PARP1 (~62% similarity in catalytic domain) and compensates for PARP-1 activity in DNA single-strand break repair[1]. Olaparib, also called as AZD2281 or Ku-0059436, one of the best investigated third-generation PARP inhibitors[2], can potently inhibit both PARP-1 (IC50=5nM) and PARP-2(IC50=1nM)[1]. BRCA1-deficient cell lines, such as MDA-MB-436 and HCC1937, were hypersensitive to olaparib than BRCA1- and BRCA2-proficient cell lines (Hs578T, MDA-MB-231 and T47D). Also olaparib shows good pharmacokinetic profiles, oral bioavailability, as well as activity in vivo[1]. These facilitate olaparib approved for use in recurrent ovarian cancer and germline BRCA HER2-negative metastatic breast cancer[2].
作用机制 Olaparib occupies the NAD binding pocket at the catalytic site, which has been proposed to trap PARP1 on DNA.[3]

Olaparib/奥拉帕尼 细胞实验

Cell Line
Concentration Treated Time Description References
HepG2 cells 50, 100, 200, 400, 800 µM 24, 48, 72, 96 hours AZD2281 inhibited the proliferation of HepG2 cells in a time- and concentration-dependent manner. Mol Med Rep. 2017 Jul;16(1):208-214.
UWB1.289 BRCA1-mutant cells 0.1 μM Evaluate the combination effect of AZD6738 with Olaparib, showing significant enhancement of cell killing in BRCA1-mutant cells. Cancer Res. 2022 Mar 15;82(6):1140-1152.
UWB1.289 +BRCA1 cells 0.1 μM Evaluate the combination effect of AZD6738 with Olaparib, showing weaker effect in BRCA1-complemented cells. Cancer Res. 2022 Mar 15;82(6):1140-1152.
LN229 15 μM 48 h To evaluate the synergistic inhibitory effect of combined treatment with Olaparib and KPT330 on the growth of GBM cells, the results showed that the combined treatment significantly inhibited cell proliferation. Autophagy. 2024 Feb;20(2):295-310.
T98G 15 μM 48 h To evaluate the synergistic inhibitory effect of combined treatment with Olaparib and KPT330 on the growth of GBM cells, the results showed that the combined treatment significantly inhibited cell proliferation. Autophagy. 2024 Feb;20(2):295-310.
E0771EGFR vIII cells 1 μM, 5 μM, 10 μM 24 or 48 h To evaluate the cytotoxicity and DNA damage effects of Olaparib on E0771EGFR vIII cells, results showed that Olaparib significantly increased DNA breaks and inhibited cell proliferation Mol Ther. 2021 Jan 6;29(1):60-74.
4T1EGFR vIII cells 1 μM, 5 μM, 10 μM 24 or 48 h To evaluate the cytotoxicity and DNA damage effects of Olaparib on 4T1EGFR vIII cells, results showed that Olaparib significantly increased DNA breaks and inhibited cell proliferation Mol Ther. 2021 Jan 6;29(1):60-74.

Olaparib/奥拉帕尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice A673 xenograft model Intraperitoneal (THZ1) and oral (olaparib) 10 mg/kg Twice daily for 40 days The combination of THZ1 and olaparib significantly inhibited tumor growth and extended survival without hematopoietic toxicity. Cancer Cell. 2018 Feb 12;33(2):202-216.e6.
Mice BRCA2-mutant TNBC PDX model Oral 50 mg/kg 5 days-on/2 days-off weekly schedule Evaluate the antitumor efficacy of AZD6738 in combination with Olaparib, showing complete tumor regression in BRCA2-mutant model. Cancer Res. 2022 Mar 15;82(6):1140-1152.
NOD-SCID mice LN229-luc mouse orthotopic xenograft model Oral 15 mg/kg Olaparib: daily, KPT330: three times a week To evaluate the anti-tumor effect of combined treatment with Olaparib and KPT330 in a GBM mouse model, the results showed that the combined treatment significantly prolonged survival and inhibited tumor growth. Autophagy. 2024 Feb;20(2):295-310.
Mice EGFR vIII-positive tumor xenograft model Intraperitoneal injection 50 mg/kg Once daily for 10 days To evaluate the anti-tumor effects of Olaparib combined with CAR-T cells on EGFR vIII-positive tumors, results showed that Olaparib significantly enhanced the anti-tumor activity of CAR-T cells and reduced MDSC recruitment Mol Ther. 2021 Jan 6;29(1):60-74.

Olaparib/奥拉帕尼 动物研究

Dose Mice: min = 10 mg/kg[4], max = 200 mg/kg[5]
Administration p.o., i.v., i.p.

Olaparib/奥拉帕尼 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02571725 Ovarian Cancer ... 展开 >> Fallopian Tube Cancer Peritoneal Neoplasms 收起 << Phase 1 Phase 2 Recruiting February 2022 United States, Florida ... 展开 >> Moffitt Cancer Center Recruiting Tampa, Florida, United States, 33612 Contact: Eleni Rokakis, BSN, RN    813-745-3593    Eleni.Rokakis@moffitt.org    United States, New Mexico Southwest Gynecologic Oncology Associates Recruiting Albuquerque, New Mexico, United States, 87106 Contact: Karen Finkelstein, MD    505-843-7813       University of New Mexico Comprehensive Cancer Center Recruiting Albuquerque, New Mexico, United States, 87131 Contact: Valerie Parks, RN    505-925-0390    vparks@salud.unm.edu    Principal Investigator: Sarah F Adams, MD          United States, Ohio The Ohio State University Recruiting Columbus, Ohio, United States, 43210 Contact: David M O'Malley, MD    614-685-6411       Contact: Molly Myers    614-685-6411    molly.myers@osumc.edu    United States, Virginia University of Virginia Cancer Center Recruiting Charlottesville, Virginia, United States, 22903 Contact: Anne Gabel    434-982-6657    am7bd@virginia.edu 收起 <<
NCT03579784 Advanced Gastric Cancer Phase 2 Recruiting April 30, 2020 Korea, Republic of ... 展开 >> Seoul National University Hospital Recruiting Seoul, Korea, Republic of, 110-744 Contact: Do-Youn Oh, MD, PhD    82-2-2072-0701    ohdoyoun@snu.ac.kr 收起 <<
NCT01972217 Metastatic Castration-resistan... 展开 >>t Prostate Cancer 收起 << Phase 2 Active, not recruiting December 31, 2018 -

Olaparib/奥拉帕尼 参考文献

[1]Menear KA, Adcock C, 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.

[2]Chen Y, Zhang L, et al. Olaparib: a promising PARP inhibitor in ovarian cancer therapy. Arch Gynecol Obstet. 2013 Aug;288(2):367-74.

[3]Murai J, Huang SY, et al. Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors. Cancer Res. 2012 Nov 1;72(21):5588-99.

Olaparib/奥拉帕尼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.51mL

2.30mL

1.15mL

23.02mL

4.60mL

2.30mL

Olaparib/奥拉帕尼 技术信息

CAS号763113-22-0
分子式C24H23FN4O3
分子量 434.46
SMILES Code O=C1NN=C(CC2=CC=C(F)C(C(N3CCN(C(C4CC4)=O)CC3)=O)=C2)C5=C1C=CC=C5
MDL No. MFCD13185161
别名 AZD2281; KU0059436
运输蓝冰
InChI Key FDLYAMZZIXQODN-UHFFFAOYSA-N
Pubchem ID 23725625
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature
溶解方案

DMSO: 105 mg/mL(241.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 2.5 mg/mL(5.75 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

DMF: 50 mg/mL(115.08 mM)，配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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

Tags: Olaparib | AZD2281;KU0059436;Olaparib. trade name Lynparza.;KU59436 | PARP | AmBeed-信号通路专用抑制剂 | Olaparib/奥拉帕尼 纯度/质量文件 | Olaparib/奥拉帕尼 亚型比较 | Olaparib/奥拉帕尼 生物活性 | Olaparib/奥拉帕尼 动物研究 | Olaparib/奥拉帕尼 临床数据 | Olaparib/奥拉帕尼 参考文献 | Olaparib/奥拉帕尼 实验方案 | Olaparib/奥拉帕尼 技术信息

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