| 货号 | 11304-100mg |
| 描述 | Poly(ADP-ribose) polymerase (PARP) is a critical DNA repair enzyme involved in DNA single-strand break repair via the base excision repair pathway. PARP1 is activated by DNA damage. Inhibiting its activity has been linked to synthetic lethality and loss of either of the breast cancer susceptibility genes, BRCA1 and BRCA2.1,2,3 BSI-201 is an irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain.1,2,4 It produces rapid apoptosis in various cancer cell lines with IC50 values ranging from 40-128 μM and is not toxic in Syrian hamsters at doses as high as 200 mg/kg.5 In phase II clinical studies, BSI-201, in combination with carboplatin and gemcitabine, has produced promising results in "triple-negative" breast cancers, increasing median overall survival from 7.7 months to 12.3 months.6 |
| 别名 | IND 71677;Iniparib; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.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). 2.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). 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.Bauer, P.I.,Mendeleyeva, J.,Kirsten, E., et al. Anti-cancer action of 4-iodo-3-nitrobenzamide in combination with buthionine sulfoximine: Inactivation of poly(ADP-ribose) polymerase and tumor glycolysis and the appearance of a poly(ADP-ribose) polymerase protease. Biochemical Pharmacology 63, 455-462 (2002). 5.Mendeleyev, J.,Kirsten, E.,Hakam, A., et al. Potential chemotherapeutic activity of 4-iodo-3-nitrobenzamide. Biochemical Pharmacology 50(5), 705-714 (1995). 6.OShaughnessy, J.,Osborne, C.,Pippen, J.E., et al. Iniparib plus chemotherapy in metastatic triple-negative breast cancer. New England Journal of Medicine 364(3), 205-214 (2011). | |
| 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 | 292.03 |
| 分子式 | C7H5IN2O3 |
| CAS号 | 160003-66-7 |
| 稳定性 | ≥ 2 years |
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