所有图片(1)
别名:
1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine, 4-[[3-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinone, AZD-2281, KU-0059436
经验公式（希尔记法）:
C24H23FN4O3
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生化/生理作用
Olaparib is an antineoplastic and potent inhibitor of poly(ADP-ribose) polymerases-1 and 2 (PARP-1, PARP-2) with an IC50 of 5 nM for PARP-1 and an IC50 of 1 nM for PARP-2. Olaparib is indicated to treat breast cancer, ovarian cancer, fallopian tube cancer, peritoneal cancer, pancreatic cancer, and prostate cancer.
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral - Repr. 1B
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Allosteric regulation of DNA binding and target residence time drive the cytotoxicity of phthalazinone-based PARP-1 inhibitors
Cell Chemical Biology, 29(12), 1694-1708 (2022)
Inhibition of PARP-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft.
Joana M Senra et al.
Molecular cancer therapeutics, 10(10), 1949-1958 (2011-10-06)
PARP-1 is a critical enzyme in the repair of DNA strand breaks. Inhibition of PARP-1 increases the effectiveness of radiation in killing tumor cells. However, although the mechanism(s) are well understood for these radiosensitizing effects in vitro, the underlying mechanism(s)
Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.
Dana V Ferraris
Journal of medicinal chemistry, 53(12), 4561-4584 (2010-04-07)
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