Olaparib-Olaparib代理/參數/廠家-生化試劑-艾美捷科技有限公司

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中文名稱: Olaparib

英文名字: Olaparib

供應商: USBiological

產品貨號: 018732

產品報價: ￥詢價/25mg ￥詢價/50mg ￥詢價/100mg

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產品描述: 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:C??H??FN?O?Molecular 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.

產品形式: 該產品為白色或類白色晶體或粉末。

保存建議: 接收到Olaparib產品后，置于-20°C溫度下保存。

其他: Usbiological公司是美國著名的抗體和生化試劑供應商，生產世界上種類最多的抗體，用于Western Blot、免疫沉淀、免疫熒光、免疫組化和流式細胞術等多種檢測方法。Usbiological公司現已擁有超過50,19234種抗體、抗原和生化產品，為科研用戶提供了諸多超值選擇。