Olaparib (AZD2281, Ku-0059436)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Olaparib（AZD2281, Ku-0059436）是一种新型的选择性PARP-1/2抑制剂。Olaparib强烈地抑制BRCA2缺陷的小鼠肿瘤细胞的生长，已经成功用于治疗含有BRCA突变的肿瘤。在异种移植非小细胞肺癌（NSCLC）细胞的裸鼠模型中，olaparib可以增加非小细胞肺癌细胞的放射敏感性。在以背轴窗室模型（dorsal window chamber (DWC) model）建立的Calu-6异种移植肺癌中，olaparib可以增加血管灌流。
参考文献：
Joana M. Senra, Brian A. Telfer, Kim E. Cherry, Cian M. McCrudden, David G. Hirst, Mark J. O’Connor, Stephen R. Wedge, and Ian J. Stratford. Inhibition of poly(ADP-ribose) polymerase-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft. Mol Cancer Ther. 2011; 10(10): 1949-1958
Bastiaan Evers, Rinske Drost, Eva Schut, Michiel Bruin, Eline vab der Burg, Patrick W. B. Derksen, Henne Holstege, Xiaoling Liu, Ellen van Drunen, H. Berna Beverloo, Graeme C. M. Smith, Niall M. B. Martin, Alan Lau, Mark J. O’Connor, and Jos Jonkers. Selective inhibition of BRCA2-deficient mammary tumor cell growth by AZD2281 and Cisplatin. Clin Cancer Res 2008; 14:3916-3925
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| Storage | Store at -20°C |
| M.Wt | 434.46 |
| Cas No. | 763113-22-0 |
| Formula | C24H23FN4O3 |
| Synonyms | AZD 2281,AZD-2281 |
| Solubility | ≥21.72 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | 4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one |
| SDF | Download SDF |
| Canonical SMILES | C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
正常LCL细胞、ATM缺失的LCL细胞 |
|
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
10 μM，1小时 |
|
应用 |
细胞对olaparib的敏感性是由共济失调毛细血管扩张突变（ATM）活性的缺失所介导的。免疫印迹分析表明，在ATM野生型，而非ATM缺失的LCLs中，olaparib以剂量依赖的方式诱导ATM依赖的靶点ATM S1981和SMC1 S966的磷酸化。 |
| 动物实验[1]： | |
|
动物模型 |
Granta-519异种移植NOD/SCID小鼠 |
|
剂量 |
50 mg/kg/d，14天；腹腔注射 |
|
应用 |
通过FACS对人CD45染色的百分比分析表明，与对照组相比，olaparib显著减少骨髓中Granta-519细胞的百分比，并减少小鼠脾脏中肿瘤细胞负荷。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Weston V J, Oldreive C E, Skowronska A, et al. The PARP inhibitor olaparib induces significant killing of ATM-deficient lymphoid tumor cells in vitro and in vivo. Blood, 2010, 116(22): 4578-4587. |
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| Olaparib (AZD2281, KU0059436)是一种有效的PARP1/2抑制剂，IC50值分别为5 nM和1 nM。. | ||||||
| 靶点 | PARP1 | PARP2 | ||||
| IC50 | 5 nM | 1 nM | ||||
质量控制和MSDS
- 批次:
化学结构
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