| 货号 | 10621-5mg |
| 描述 | Many of the products generated by alkylating agents on DNA can be efficiently repaired by normal base excision repair (BER).1 Some poly(ADP-ribose) polymerases (PARPs) assist in the repair of single-strand DNA nicks, an important step in BER.2 Olaparib is a potent inhibitor of PARP1 and PARP2 (IC50 = 5 and 1 nM, respectively) but is less effective against the PARP tankyrase-1 (IC50 = 1.5 µM).3 It can be used in cells and in animals, alone or in combination therapy with alkylating agents, to block BER and increase cancer cell death.3,4,5,6 |
| 别名 | AZD 2281;Ku-0059436; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Rowe, B.P., and Glazer, P.M. Emergence of rationally designed therapeutic strategies for breast cancer targeting DNA repair mechanisms. Breast Cancer Research 12(2), 1-11 (2010). 2.Davar, D.,Beumer, J.H.,Hamieh, L., et al. Role of PARP inhibitors in cancer biology and therapy. Current Medicinal Chemistry 19(23), 3907-3921 (2012). 3.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-1. J. Med. Chem. 51(20), 6581-6591 (2008). 4.Yuan, Y.,Liao, Y.M.,Hsueh, C.T., et al. Novel targeted therapeutics: Inhibitors of MDM2, ALK and PARP. J. Hematol. Oncol. 4(16), 1-14 (2011). 5.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). 6.Javle, M., and Curtin, N.J. The potential for poly (ADP-ribose) polymerase inhibitors in cancer therapy. Ther. Adv. Med. Oncol. 3(6), 257-267 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 434.5 |
| 分子式 | C24H23FN4O3 |
| CAS号 | 763113-22-0 |
| 稳定性 | ≥ 2 years |
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