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Biological Activity:
Highly potent, oral and selective inhibitor of poly(ADP-ribose) polymerase (PARP); with IC50 = 5nM (PARP-1) and 1 nM (PARP-2). It blocks enzymes that repair DNA damage caused by cancer treatments such as radiation and drugs.
References: online
S Vasiliou et al. Olaparib. Drugs of the Future. 2009, 34(2), 101.
KA Menear 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. [online]
S Rottenberg et al. High sensitivity of BRCA1-deficient mammary tumors to the PARP inhibitor AZD2281 alone and in combination with platinum drugs. Proc. Nat. Acad. Sci. USA, 2008, 105(44), 17079–84. [online]
T Hay et al. Poly(ADP-ribose) polymerase-1 inhibitor treatment regresses autochthonous Brca2/p53-mutant mammary tumors in vivo and delays tumor relapse in combination with carboplatin. Cancer Res. 2009, 69(9), 3850. [online]
C Mitchell et al. Poly(ADP-Ribose) Polymerase 1 Modulates the Lethality of CHK1 Inhibitors in Carcinoma Cells. Mol. Pharmacol. 2010, 78(5), 909-917. [online]
Chemical Name: 4-[(3-{[4-Cyclopropylcarbonyl)piperazin-4-yl]carbonyl}-4-fluorophenyl)methyl]phtalazin-1(2H)-one
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