- 中文名称
Olaparib
- 英文名字
- Olaparib
- 供应商
- USBiological
- 产品货号
- 018732
- 产品报价
- ¥询价/25mg ¥询价/50mg ¥询价/100mg
- 产品说明书
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- 产品新闻
- 背景资料
- USBiological品牌是全球有名的抗原抗体和生化试剂供应商,生产世界上种类最多的抗体,用于Western Blot、免疫沉淀、免疫荧光、免疫组化和流式细胞术等多种检测方法。武汉艾美捷科技作为USBiological品牌中国区域总代理,是行业中少有的致力于服务客户,帮助客户,且拥有独立的专业销售团队、技术支持团队、市场营销团队、进出口报关团队的高科技生物企业。可以为您提供及时的咨询响应,专业的产品和解决方案支持,稳健快捷的交货周期,优质放心的售后服务。我们致力于为您提供有价值的产品和服务,在意您的成功!
- 产品描述
- Olaparib is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Olaparib has been shown to induce significant killing of ATM-deficient lymphoid tumor cells in vitro and in vivo. Recent studies show that Olaparib increases radiosensitivity of a lung tumor xenograft, making it a potential candidate for use in combination with radiotherapy.PARP1 acts as a critical molecule in the repair of DNA single-strand breaks (SSBs) and plays an important role in maintaining DNA integrity. de Murcia, J., et al. "Requirement of poly(ADP-ribose) polymerase in recovery from DNA damage in mice and in cells." Proc. Natl. Acad. Sci. USA 94: 7303-7307 (1997).PARP inhibitors inhibit PARP1 during S-phase and induce inactivation of SSB repair and thus cause DNA double-strand breaks, which induces BRCA-deficient cancer cell apoptosis. Bryant, H.E., et al. "Specific killing of BRCA2-deficient tumours with inhibitors of poly(ADP-ribose) polymerase." Nature 434: 913-917 (2005). Farmer, H., et al. "Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy." Nature 434: 917-921 (2005).The PARP inhibitor olaparib was tested in a genetically engineered mouse model for BRCA1-associated breast cancer. Olaparib inhibited tumor growth and significantly improved survival without signs of toxicity. Rottenberg, S., et al. "High sensitivity of BRCA1-deficient mammary tumors to the PARP inhibitor AZD2281 alone and in combination with platinum drugs." Proc. Natl. Acad. Sci. USA 105: 17079-17084 (2008).Long-term treatment with olaparib caused the development of drug resistance, which was induced by up-regulation of Abcb1a/b genes encoding P-glycoprotein efflux pumps. The resistance to olaparib could be overcome by tariquidar, a P-glycoprotein inhibitor. Rottenberg, S., et al. "High sensitivity of BRCA1-deficient mammary tumors to the PARP inhibitor AZD2281 alone and in combination with platinum drugs." Proc. Natl. Acad. Sci. USA 105: 17079-17084 (2008).Combination treatment using olaparib with cisplatin or carboplatin improved the recurrence-free and overall survival in a murine model, indicating that olaparib enhances the effect of these DNA-damaging agents. Rottenberg, S., et al. "High sensitivity of BRCA1-deficient mammary tumors to the PARP inhibitor AZD2281 alone and in combination with platinum drugs." Proc. Natl. Acad. Sci. USA 105: 17079-17084 (2008).Olaparib inhibited the growth of BRCA2-deficient versus BRCA2-proficient mammary tumor cells. Combination treatment of olaparib and cisplatin had a synergistic cytotoxicity against BRCA2-deficient cells but not against BRCA2-proficient control cells. Evers, B., et al. "Selective inhibition of BRCA2-deficient mammary tumor cell growth by AZD2281 and cisplatin." Clin. Cancer Res. 14: 3916-3925 (2008).Synonyms:4-[[3-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinone; AZD-2281; KU 0059436; KU-59436; 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazineCAS Number:763113-22-0Molecular Formula:C₂₄H₂₃FN₄O₃Molecular Weight:434.46Appearance:Supplied as a white to off-white, cystalline or powderPurity:≥99% (HPLC, TLC)Solubility:Soluble in DMSO at 33mg/ml; soluble in ethanol at 1.7mg/ml with slight warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20uM buffers, serum, or other additives may increase or decrease the aqueous solubility.Melting Point:208-209ºCElemental Analysis:Calculated:%C: 66.35%%H: 5.34%%F: 4.37%%N: 12.90%Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 6 months after receipt at -20°C. Reconstitute with DMSO. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap.Important Note: This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological. Toxicity and Hazards: All products should be handled by qualified personnel only, trained in laboratory procedures.
- 产品形式
- 该产品为白色或类白色晶体或粉末。
- 保存建议
- 接收到Olaparib产品后,置于-20°C温度下保存。
- 其他
- Usbiological公司是美国著名的抗体和生化试剂供应商,生产世界上种类最多的抗体,用于Western Blot、免疫沉淀、免疫荧光、免疫组化和流式细胞术等多种检测方法。Usbiological公司现已拥有超过50,19234种抗体、抗原和生化产品,为科研用户提供了诸多超值选择。
- 注意
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