Olaparib

SKU: orb1304620

特色

描述

Olaparib is a potent, selective, and orally bioavailable inhibitor of PARP1 and PARP2, with significantly weaker activity against tankyrase-1. It is widely used in cancer research, particularly in studies of BRCA-deficient tumors, and has been shown to induce autophagy and mitophagy in both cellular and animal models.

研究领域

Cell Biology, Epigenetics & Chromatin, Molecular Biology, Pharmacology & Drug Discovery

图片与验证

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关键属性

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CAS 号	763113-22-0
MW	434.46
纯度	99.99% (May vary between batches)
分子式	C₂₄H₂₃FN₄O₃
SMILES	C(C=1C=2C(C(=O)NN1)=CC=CC2)C3=CC(C(=O)N4CCN(C(=O)C5CC5)CC4)=C(F)C=C3
靶点	Mitophagy, Autophagy, PARP
溶解性	10% DMSO+40% PEG300+5% Tween 80+45% Saline:8 mg/mL (18.41 mM);H2O:< 1 mg/mL (insoluble);DMSO:82.5 mg/mL (189.89 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

客户验证数据

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以下数据由各地研究人员提交。即使我们尚未自行检测，这些结果也有助于判断该产品是否适合您的应用或种属。

按应用统计成功数

反应性分布

最新实验

16 Results

稀释

样本

摘要

In vitro

Human

Human ovarian cancer cells (specifically OVCAR 5 line)

It was applied to evaluate its...

In vivo

Mouse

80 or 100 mg/kg

Mice bearing patient-derived xenografts (PDXs)

Olaparib was administered orally to mice...

In vitro

Human

Human breast cancer cell lines (MCF7, MDA-MB-231, SK-BR-3, HCC1937, T47D, HCC1806)

Olaparib was dissolved in DMSO and...

In vivo

Mouse

100 mg/kg

BALB/c nude mice bearing subcutaneous MCF7AR or MDA-MB-231 xenografts

Olaparib was dissolved in carboxymethylcellulose sodium...

In vitro

Mouse

30 nM - 30 μM

Murine (Panc02, KPC-A548) pancreatic cancer cell lines

Olaparib were dissolved in DMSO to...

生物活性

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靶点 IC50	PARP1:5 nM (cell free)\|PARP2:1 nM (cell free)\|tankyrase 1:1.5 μM
体内	METHODS: To detect anti-tumor activity in vivo, Olaparib (10 mg/kg) and TMZ (50 mg/kg) were orally administered to mice bearing human colorectal cancer tumor SW620 once daily for five days. RESULTS: Significant suppression of tumor volume was observed in the TMZ plus Olaparib combination treatment group compared to the TMZ group alone. METHODS: To investigate the therapeutic effects of Olaparib on asthma, Olaparib (1-10 mg/kg) was administered intraperitoneally once daily for three days to an OVA-based asthmatic C57BL/6 mouse model. RESULTS: Olaparib significantly reduced airway eosinophilia, mucus production, and hyperresponsiveness. The protective effects of Olaparib were associated with inhibition of the Th2 cytokines eotaxin, IL-4, IL-5, IL-6, IL-13, and M-CSF, as well as ovalbumin-specific IgE, and an increase in the Th1 cytokine IFN-γ. Olaparib is a potential candidate for clinical trials in human asthma.
体外	METHODS: Human cervical cancer cells SiHa and ME180 were treated with Olaparib (5-10 µM) and cisplatin (1-30 µM) for 72 h. Cell growth inhibition was detected by MTT. RESULTS: Olaparib and cisplatin co-treatment showed significant cell growth inhibition compared to cells treated with a single drug. METHODS: Human endometrial cancer cells HEC-6 and HEC-6-PTEN were treated with Olaparib (10 μM) for 72 h. The cell cycle was analyzed by Flow Cytometry. RESULTS: Olaparib induced a significant increase in the sub-G1 population of HEC-6 and HEC-6-PTEN cells. METHODS: Chicken lymphoma cells DT40 were treated with Olaparib (0.01-10 μM) for 30 min, and the expression levels of target proteins were detected by Western Blot. RESULTS: Olaparib dose-dependently inhibited the expression level of PARylation and the activation of PARP.
细胞研究	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 .
动物研究	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 .

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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Autophagy, AZD 2281, AZD2281, AZD-2281, PARP, PARP1, PARP2, Mitophagy, Mitochondrial Autophagy, Olaparib, orally, poly ADP ribose polymerase, inhibit, Inhibitor, KU 0059436, KU0059436, KU-0059436

相似产品

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BER-IN-1 [orb3173060]
可选规格： 50 mg, 10 mg
PARP1-IN-44 [orb3173354]
可选规格： 50 mg, 10 mg
Polθ-IN-9 [orb3174197]
CAS 号：
3050552-13-8
MW:
624.05
分子式：
C₃₀H₃₁ClF₅N₅O₂
可选规格： 10 mg, 50 mg
BRCA2-RAD51-IN-2 [orb3028169]
可选规格： 50 mg, 10 mg
PARP1 degrader 1 [orb3181792]
可选规格： 50 mg, 10 mg

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

23725625 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

CAS 号：	3050552-13-8
MW:	624.05
分子式：	C₃₀H₃₁ClF₅N₅O₂

Olaparib

描述

研究领域

图片与验证

关键属性

客户验证数据

按应用统计成功数

反应性分布

最新实验

生物活性

储存与操作

别名

相似产品

BER-IN-1 [orb3173060]

PARP1-IN-44 [orb3173354]

Polθ-IN-9 [orb3174197]

BRCA2-RAD51-IN-2 [orb3028169]

PARP1 degrader 1 [orb3181792]

质量保证

化合物标识

关键属性

实验方案信息

可选规格