Cat. No. Name Size Price Add Cart
KI1184AZD228150 mg$260
AZD2281100 mg$390
AZD2281500 mg$507
AZD2281500 mg$2032

Chemical Characteristic

Product NameAZD2281
SynonymsKU-0059436, Olaparib
CAS No.763113-22-0
Molecular Weight 434.47
FormulaC24H23FN4O3
Chemical Name4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one
SmilesN1(CCN(CC1)C(=O)c1c(ccc(c1)Cc1n[nH]c(=O)c2ccccc12)F)C(=O)C1CC1
Chemical Structure

Biological activities

AZD2281 is a poly ADP-ribose polymerase (PARP) inhibitor. The IC50 of AZD2281 is 5 and 1 nM against PARP1 and PARP2, respectively. In addition, AZD2281 also inhibits tankyrase-1 with an IC50 of 1.5 µM. AZD2281 exhibits standalone activity against BRCA1-deficient breast cancer cell lines and SW620 cells. [1] AZD2281 generates strong differential growth inhibition of BRCA2-deficient versus BRCA2-proficient mammary tumor cells.[2] AZD2281 dose-dependently induces the phosphorylation of the ATM-dependent targets ATM S1981 and SMC1 S966. [3] AZD2281 increases the cytotoxic effects of radiation in irradiated Calu-6 and A549 cells.[4] The combination of AZD2281 and temozolomide generates a considerable inhibition of tumor volumes as compared with that of the temozolomide alone group in an SW620 colorectal cancer xenograft model.[1] AZD2281 significantly reduces the percentage of Granta-519 cells in the bone marrow and a trend toward reduced tumor cell load in the spleen of mice.[3] The combination of AZD2281 with fractionated radiotherapy significantly produces tumor regression in Calu-6 xenografts.[4] AZD2281 markedly decreases tumor growth and prolongs 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 with the ATM-proficient cell line Z138.[5]

Protocols

In vivo: AZD2281 is dissolved in phosphate buffered saline (PBS) containing 10% DMSO and 10% 2-hydroxy-propyl-β-cyclodextrin.[4]

References

[1] Menear KA, et al. 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008, 51(20): 6581-6591.
[2] Evers B, et al. Selective inhibition of BRCA2-deficient mammary tumor cell growth by AZD2281 and cisplatin. Clin Cancer Res. 2008, 14(12): 3916-3925.
[3] Weston VJ, 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.
[4] Senra JM, et al. Inhibition of PARP-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft. Mol Cancer Ther. 2011, 10(10): 1949-1958.
[5] Williamson CT, et al. ATM deficiency sensitizes mantle cell lymphoma cells to poly(ADP-ribose) polymerase-1 inhibitors. Mol Cancer Ther. 2010, 9(2): 347-357.

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