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Olaparib(AZD2281)
Cat No.
CEI-0329
Description
Olaparib(AZD2281) can inhibit PARP1 and PARP2 with IC50 of 5 nM and 1 nM.
Alias
KU-0059436
CAS No.
763113-22-0
Molecular Weight
434.469
Purity
>99%
Storage
2 years at -20centigrade Powder
Synonyms
KU-0059436
Targets
PARP1, PARP2
Molecular Formula
C24H23FN4O3
Chemical Name
4-(3-(1-(cyclopropanecarbonyl)piperazine-4-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
Solubility
DMSO 87 mg/mL Water
In vitro
Olaparib(AZD2281, KU0059436) is a selective inhibitor, which can potently inhibit PARP-1 and PARP-2 enzymes with IC50 of 5 nM and 1 nM, respectively.Treatment of these cell lines with 11 different anticancer drugs or with gamma-irradiation showed that AZD2281, a novel and specific PARP inhibitor, caused the strongest differential growth inhibition of BRCA2-deficient versus BRCA2-proficient mammary tumor cells. Synergistic cytotoxicity of AZD2281 and cisplatin against BRCA2-deficient cells but not against BRCA2-proficient control cells.
In vivo
AZD2281 significantly decreased tumor growth and increased overall survival in mice bearing s.c. xenografts of ATM-deficient Granta-519 cells while producing only a modest effect on overall survival of mice bearing xenografts of the ATM-proficient cell line, Z138. Olaparib as maintenance treatment significantly improved progression-free survival among patients with platinum-sensitive, relapsed, high-grade serous ovarian cancer.
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