Olaparib
PARP1 inhibitor / A highly potent and selective PARP-inhibitor with IC₅₀ values of 5 nM and 1 nM for PARP-1 and PARP-2, respectively.1 In a genetically engineered mouse model for BRCA1-associated breast cancer olaparib inhibited tumor growth and improved survival with no signs of toxicity.2 Synergizes with many other anticancer agents.3 Shows efficacy in colorectal cancers.4 Prevents house dust mite allergen-induced asthma in a mouse model.5
Biochemicals & reagents
763113-22-0
AZD-2281; KU-59436
1) Menear et al. (2008), 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. 51 6581 2) Rottenberg et al. (2008), 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 3) Avila-Arroyo et al. (2015), Synergistic effect of Trabectedin and Olaparib combination regimen in breast cancer cell lines; J.Breast Cancer 18 329 4) Xu et al. (2015), Combined olaparib and oxaliplatin inhibits tumor proliferation and induces G2/M arrest and γ-H2AX foci formation in colorectal cancer; Onco.Targets Ther. 8 3047 5) Ghonim et al. (2015), PARP is activated in human asthma and its inhibition by olaparib blocks house dust mite-induced disease in mice; Clin.Sci.(Lond) 129 951
-20°C
TARGET: PARP -- PATHWAY: DNA repair -- DISEASE AREA: Cancer; Inflammation