Olaparib-d4

Olaparib-d₄ is intended for use as an internal standard for the quantification of olaparib by GC- or LC-MS. Olaparib is a potent inhibitor of PARP1 and PARP2 (IC₅₀s = 5 and 1 nM, respectively) but is less effective against the PARP tankyrase-1 (IC₅₀ = 1.5 µM).¹ It can be used in cells and in animals, alone or in combination therapy with alkylating agents, to block base excision repair and increase cancer cell death.^1,2,3,4

1.Menear, K.A., Adcock, C., Boulter, R., et al.4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: A novel bioavailable inhibitor of Poly(ADP-ribose) polymerase-1J. Med. Chem.51(20)6581-6591(2008) 2.Yuan, Y., Liao, Y.M., Hsueh, C.T., et al.Novel targeted therapeutics: Inhibitors of MDM2, ALK and PARPJ. Hematol. Oncol.4(16)1-14(2011) 3.Plummer, R.Poly(ADP-ribose) polymerase inhibition: A new direction for BRCA and triple-negative breast cancer•Breast Cancer Res.13(4)1-6(2011) 4.Javle, M., and Curtin, N.J.The potential for poly (ADP-ribose) polymerase inhibitors in cancer therapyTher. Adv. Med. Oncol.3(6)257-267(2011)