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Olaparib

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产品编号 T3015Cas号 763113-22-0
别名 奥拉帕尼, KU0059436, AZD2281

Olaparib (KU0059436) 是 PARP1/PARP2 的小分子抑制剂 (IC50=5/1 nM),对 PARP tankyrase-1 的抑制活性较弱 (IC50=1.5 μM),具有选择性和口服活性。Olaparib 具有自噬和线粒体自噬激活活性。

Olaparib

Olaparib

Rating icon 很棒
纯度: 100%
产品编号 T3015 别名 奥拉帕尼, KU0059436, AZD2281Cas号 763113-22-0

Olaparib (KU0059436) 是 PARP1/PARP2 的小分子抑制剂 (IC50=5/1 nM),对 PARP tankyrase-1 的抑制活性较弱 (IC50=1.5 μM),具有选择性和口服活性。Olaparib 具有自噬和线粒体自噬激活活性。

规格价格库存数量
5 mg¥ 265现货
10 mg¥ 396现货
50 mg¥ 995现货
100 mg¥ 1,597现货
200 mg¥ 2,398现货
500 mg¥ 3,997现货
1 g¥ 5,500现货
1 mL x 10 mM (in DMSO)¥ 282现货
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产品介绍

生物活性
产品描述
Olaparib (KU0059436) is a small molecule inhibitor of PARP1/PARP2 (IC50=5/1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.
靶点活性
PARP2:1 nM (cell free), PARP1:5 nM (cell free)
体外活性
方法:人子宫颈癌细胞 SiHa 和 ME180 用 Olaparib (5-10 µM) 和 cisplatin (1-30 µM) 处理 72 h,使用 MTT 方法检测细胞生长抑制情况。
结果:Olaparib 和 cisplatin 共同处理比用单一药物处理的细胞显示出显著的细胞生长抑制作用。[1]
方法:人子宫内膜癌细胞 HEC-6 和 HEC-6-PTEN 用 Olaparib (10 μM) 处理 72 h,使用 Flow Cytometry 方法分析细胞周期情况。
结果:Olaparib 诱导 HEC-6 和 HEC-6-PTEN 细胞显著增加了亚 G1 群体。[2]
方法:鸡淋巴瘤细胞 DT40 用 Olaparib (0.01-10 μM) 处理 30 min,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:Olaparib 剂量依赖性抑制 PARylation 的表达水平,抑制 PARP 的活化。[3]
体内活性
方法:为检测体内抗肿瘤活性,将 Olaparib (10 mg/kg) 和 TMZ (50 mg/kg) 口服给药给携带人结直肠癌肿瘤 SW620 的小鼠,每天一次,持续五天。
结果:与单独 TMZ 组相比,TMZ 加 Olaparib 组合治疗组观察到肿瘤体积的显著抑制。[4]
方法:为研究 Olaparib 对哮喘的治疗作用,将 Olaparib (1-10 mg/kg) 腹腔注射给基于 OVA 的哮喘 C57BL/6 小鼠模型,每天一次,持续三天。
结果:Olaparib 能显著减少气道嗜酸性粒细胞增多、粘液产生和高反应性。Olaparib 的保护作用与抑制 Th2 细胞因子 eotaxin、IL-4、IL-5、IL-6、IL-13 和 M-CSF 以及卵清蛋白特异性 IgE 有关,同时增加 Th1 细胞因子 IFN-γ。Olaparib 有可能成为人类哮喘临床试验的候选药物。[5]
激酶实验
This assay determined the ability of test compounds to inhibit PARP-1 enzyme activity. The method that was used was as reported. We measured PARP-2 activity inhibition by using a variation of the PARP-1 assay in which PARP-2 protein (recombinant) was bound down by a PARP-2 specific antibody in a 96-well white-walled plate. PARP-2 activity was measured following 3H-NAD+ DNA additions. After washing, scintillant was added to measure 3 H-incorporated ribosylations. For tankyrase-1, an AlphaScreen assay was developed in which HIS-tagged recombinant TANK-1 protein was incubated with biotinylated NAD+ in a 384-well ProxiPlate assay. Alpha beads were added to bind the HIS and biotin tags to create a proximity signal, whereas the inhibition of TANK-1 activity was directly proportional to the loss of this signal. All experiments were repeated at least three times [1].
细胞实验
HSC-2, Ca9-22, and SAS oral carcinoma cells were seeded in 24-well plates at a density of 2 × 104 cells/well. After overnight incubation, the culture medium was replaced with fresh medium containing various concentrations of PARP inhibitor AZD228 or cisplatin. After 24 h of treatment, the number of viable cells was assessed using an MTT assay as reported previously. Briefly, one-tenth of the fluid volume of 5 mg/mL MTT in RPMI-1640 medium was added to each well, followed by incubation for 4 h at 37 °C. After incubation, the medium was carefully removed and an adequate volume of 0.1 N HCl in isopropanol was added to each well and the resultant formazan crystals was dissolved. Absorbance was determined at 570 nm by microplate reader in 96-well assay plates. All experiments were performed in triplicate [2].
动物实验
Once the tumor diameter had reached 7 mm, the mice were randomly assigned to the following groups: (a) control (200 μL saline); (b) cisplatin (2 mg/kg per body weight, dissolved in 200 μL sterilized water); (c) AZD2281 (25 mg/kg per body weight, dissolved in 200 μL sterilized water); or (d) combination (both cisplatin and AZD2281). The chemicals were administered intraperitoneally every three days, five times. Although AZD2281 is administered orally in the clinic, intraperitoneal injection was recommended by the manufacturer because of easier manipulation and the ethical constraints associated with oral gavage administration to mice. Tumor size and body weight were measured at the time of administration. The tumor volume was calculated using following equation. Tumor volume = verticality × width × height × 0.5236. Three days after the last administration, all surviving mice were sacrificed [2].
别名奥拉帕尼, KU0059436, AZD2281
化学信息
分子量434.46
分子式C24H23FN4O3
CAS No.763113-22-0
SmilesC(C=1C=2C(C(=O)NN1)=CC=CC2)C3=CC(C(=O)N4CCN(C(=O)C5CC5)CC4)=C(F)C=C3
密度1.43
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 50 mg/mL (115.09 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 8 mg/mL (18.41 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
溶液配制表
1mg5mg10mg50mg
1 mM2.3017 mL11.5085 mL23.0171 mL115.0854 mL
5 mM0.4603 mL2.3017 mL4.6034 mL23.0171 mL
10 mM0.2302 mL1.1509 mL2.3017 mL11.5085 mL
1mg5mg10mg50mg
20 mM0.1151 mL0.5754 mL1.1509 mL5.7543 mL
50 mM0.0460 mL0.2302 mL0.4603 mL2.3017 mL
100 mM0.0230 mL0.1151 mL0.2302 mL1.1509 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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