| 货号 | 11570-1mg |
| 描述 | Poly(ADP-ribose) polymerases (PARPs) are activated by DNA single- and double-strand breaks and promote repair of DNA damage through the relaxation of chromatin and recruitment of other repair proteins.1,2,3 Inhibition of PARP activity has been linked to synthetic lethality in cells with mutations in BRCA1orBRCA24 and is used as a therapeutic strategy to selectively target cancers.5 Rucaparib is a potent, cell-permeable inhibitor of PARP1 (Ki=<5 nM) that is used in clinical therapy to sensitize cancer cells to chemotherapy.6,7 Rucaparib inactivates PARP activity in cells with homologous recombination DNA repair pathway mutations at LC50 values ranging from 1.3-5.5 μM.7 At 25 mg/kg, rucaparib arrests tumor growth in mice bearing epigenetically silenced BRCA1 UACC3199 xenograft tumors.7 It has been shown to increase efficacy of temozolomide in medulloblastoma cells and xenografts.6 Rucaparib (phosphate) is the phosphate salt of rucaparib (Item No. 15643) and has improved aqueous solubility. |
| 别名 | AG-014699;PF-01367338; |
| 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.Johnson, N.,Li, Y.C.,Walton, Z.E., et al. Compromised CDK1 activity sensitizes BRCA-proficient cancers to PARP inhibition. Nature Medicine 17(7), 875-882 (2011). 5.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). 6.Daniel, R.A.,Rozanska, A.L.,Mulligan, E.A., et al. Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. Br. J. Cancer 103(10), 1588-1596 (2010). 7.Drew, Y.,Mulligan, E.A.,Vong, W.T., et al. Therapeutic potential of poly(ADP-ribose) polymerase inhibitor AG014699 in human cancers with mutated or methylated BRCA1 or BRCA2. JNCI 103(4), 334-346 (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 | 421.4 |
| 分子式 | C19H18FN3O • H3PO4 |
| CAS号 | 459868-92-9 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |