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A neuropeptide with diverse biological activities
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)
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