| 货号 | 20842-1mg |
| 描述 | MK-4827 is an orally bioavailable inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 3.8 and 2.1 nM, respectively).1 It inhibits the proliferation of cancer cells carrying the breast cancer mutations BRCA1 and BRCA2 in vitro(IC50 values range from 10-100 nM) and has efficacy alone against a xenograft of BRCA1-deficient cancer in mice.1,2 MK-4827 sensitizes human lung and breast cancer xenografts to radiation in mice.3 Formulations containing MK-4827 are effective against ovarian cancer, particularly in platinum-sensitive, recurrent ovarian cancer.4 |
| 别名 | Niraparib tosylate; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Jones, P.,Altmura, S.,Boueres, J., et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): A novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J. Med. Chem. 52(22), 7170-7185 (2009). 2.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). 3.Wang, L.,Mason, K.A.,Ang, K.K., et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs 30(6), 2113-2120 (2012). 4.Mirza, M.R.,Monk, B.J.,Herrstedt, J., et al. Niraparib maintenance therapy in platinum-sensitive, recurrent ovarian cancer. N. Engl. J. Med. 375(22), 2154-2164 (2016). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 492.6 |
| 分子式 | C19H20N4O • C7H8O3S |
| CAS号 | 1038915-73-9 |
| 稳定性 | ≥ 2 years |
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