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奥拉帕尼 /Olaparib 98%

货号:A134565 同义名: AZD2281;KU0059436 Ambeed 开学季,买赠积分,赢豪礼

Olaparib 是一种 PARP 抑制剂,对 PARP1PARP2 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 化学结构 CAS号:763113-22-0
Olaparib 化学结构
CAS号:763113-22-0
Olaparib 3D分子结构
CAS号:763113-22-0
Olaparib 化学结构 CAS号:763113-22-0
Olaparib 3D分子结构 CAS号:763113-22-0
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Olaparib 纯度/质量文件 产品仅供科研

货号:A134565 标准纯度: 98%
批次查询: 批次纯度:

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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

97%
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

98+%
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 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 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
5637 Growth Inhibition Assay IC50=7.9286 μM SANGER
697 Growth Inhibition Assay IC50=2.84173 μM SANGER
769-P Growth Inhibition Assay IC50=24.8466 μM SANGER
8505C Growth Inhibition Assay IC50=26.4977 μM SANGER

Olaparib 动物研究

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

Olaparib 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 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 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 技术信息

CAS号763113-22-0
分子式C24H23FN4O3
分子量 434.46
别名 AZD2281;KU0059436;Olaparib. trade name Lynparza.;KU59436
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

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

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 45 mg/mL suspension

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