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Olaparib

Olaparib

产品编号 T3015   CAS 763113-22-0
别名: AZD2281, 奥拉帕尼, KU0059436

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。

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Olaparib Chemical Structure
Olaparib, CAS 763113-22-0
规格 价格/CNY 货期 数量
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 * 10 mM (in DMSO) ¥ 282 现货
其他形式的 Olaparib:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: Olaparib (T3015)
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生物活性
化学信息
存储 & 溶解度
参考文献
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 AZD2281, 奥拉帕尼, KU0059436
化合物与蛋白结合的复合物

T3015_2

HUMAN ARTD2 (PARP2) - CATALYTIC DOMAIN IN COMPLEX WITH OLAPARIB

分子量 434.46
分子式 C24H23FN4O3
CAS No. 763113-22-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 80 mg/mL (184.1 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3017 mL 11.5085 mL 23.0171 mL 57.5427 mL
5 mM 0.4603 mL 2.3017 mL 4.6034 mL 11.5085 mL
10 mM 0.2302 mL 1.1509 mL 2.3017 mL 5.7543 mL
20 mM 0.1151 mL 0.5754 mL 1.1509 mL 2.8771 mL
50 mM 0.046 mL 0.2302 mL 0.4603 mL 1.1509 mL
100 mM 0.023 mL 0.1151 mL 0.2302 mL 0.5754 mL

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TargetMol Library Books参考文献

1. Prasad CB, et al. Olaparib modulates DNA repair efficiency, sensitizes cervical cancer cells to cisplatin and exhibits anti-metastatic property. Sci Rep. 2017 Oct 9;7(1):12876. 2. Miyasaka A, et al. Anti-tumor activity of olaparib, a poly (ADP-ribose) polymerase (PARP) inhibitor, in cultured endometrial carcinoma cells. BMC Cancer. 2014 Mar 13;14:179. 3. Murai J, et al. Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors. Cancer Res. 2012 Nov 1;72(21):5588-99. 4. Menear KA, 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. 5. Ghonim MA, et al. PARP inhibition by olaparib or gene knockout blocks asthma-like manifestation in mice by modulating CD4(+) T cell function. J Transl Med. 2015 Jul 14;13:225.

TargetMol Library Books文献引用

1. Long X, Dai A, Huang T, et al.Simultaneous Delivery of Dual Inhibitors of DNA Damage Repair Sensitizes Pancreatic Cancer Response to Irreversible Electroporation.ACS nano.2023 2. Valentini E, Di Martile M, Brignone M, et al.Bcl-2 family inhibitors sensitize human cancer models to therapy.Cell Death & Disease.2023, 14(7): 441. 3. Pan X, Zhang W, Wang L, et al.KLF12 transcriptionally regulates PD‐L1 expression in non‐small cell lung cancer.Molecular Oncology.2023 4. Zhao J, Xu J, Wu M, et al.LncRNA H19 Regulates Breast Cancer DNA Damage Response and Sensitivity to PARP Inhibitors via Binding to ILF2.International Journal of Molecular Sciences.2023, 24(11): 9157. 5. Yu L, Zhou D, Zhang G, et al. Co‐occurrence of BAP1 and SF3B1 mutations in uveal melanoma induces cellular senescence. Molecular Oncology.. 2022, 16(3): 607-629. 6. Malka M M, Eberle J, Niedermayer K, et al. Dual PARP and RAD51 Inhibitory Drug Conjugates Show Synergistic and Selective Effects on Breast Cancer Cells. Biomolecules. 2021, 11(7): 981. 7. Du T, Zhang Z, Zhou J, et al. A Novel PARP Inhibitor YHP-836 For the Treatment of BRCA-Deficiency Cancers. Frontiers in pharmacology. 2022, 13. 8. Dai W, Wu J, Peng X, et al. CDK12 orchestrates super‐enhancer‐associated CCDC137 transcription to direct hepatic metastasis in colorectal cancer. Clinical and Translational Medicine. 2022, 12(10): e1087. 9. Guffanti F, Alvisi M F, Anastasia A, et al. Basal expression of RAD51 foci predicts olaparib response in patient-derived ovarian cancer xenografts. British Journal of Cancer. 2021: 1-9. 10. Wu Y, Wu T, Hu X, et al. Proguanil synergistically sensitizes ovarian cancer cells to olaparib by increasing DNA damage and inducing apoptosis. International Journal of Medical Sciences. 2022, 19(2): 233-241.
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相关化合物库

该产品包含在如下化合物库中:
EMA 上市药物库 抗癌上市药物库 药物功能重定位化合物库 抗癌药物库 抗癌临床化合物库 抗癌活性化合物库 高选择性抑制剂库 抑制剂库 DNA 损伤和修复分子库 抗乳腺癌化合物库

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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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Olaparib 763113-22-0 Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair Mitophagy PARP AZD2281 Mitochondrial Autophagy inhibit orally Inhibitor 奥拉帕尼 PARP1 KU0059436 poly ADP ribose polymerase PARP2 KU 0059436 AZD-2281 AZD 2281 KU-0059436 inhibitor

 

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