AZD 7762
货号：
11491-1mg 基本售价：
294.0 元 规格：
1 mg
产品信息
概述| 货号 | 11491-1mg |
| 描述 | Actively proliferating cells experience blocks at certain checkpoints in the cell cycle when DNA damage is detected. These checkpoints allow for DNA damage repair before further cell cycle progression. Targeting signaling pathways to selectively inhibit repair at these checkpoints in tumor cells is of considerable interest to cancer therapeutics. AZD 7762 selectively inhibits the activity of checkpoint kinases (Chk) 1 and Chk2 (IC50s = 5 nM) by competitively and reversibly binding their respective ATP-binding sites (Ki = 3.6 nM for Chk1).1 AZD 7762 abrogates DNA damage-induced S and G2 checkpoints with an EC50 value of 10 nM and potentiates the efficacy of DNA-damage repair prohibitive agents, gemcitabine and topotecan, both in vitro and in various tumor xenografts by modulating downstream checkpoint pathway proteins.1,2,3 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Zabludoff, S.D.,Deng, C.,Grondine, M.R., et al. AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. Molecular Cancer Therapeutics 7, 2955-2966 (2008).
2.Mitchell, J.B.,Choudhuri, R.,Fabre, K., et al. In vitro and in vivo radiation sensitization of human tumor cells by a novel checkpoint kinase inhibitor, AZD7762. Clinical Cancer Research 16(7), 2076-2084 (2010).
3.Morgan, M.A.,Parsels, L.A.,Zhao, L., et al. Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair. Cancer Research 70(12), 4972-4981 (2010).
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| 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 | 362.4 |
| 分子式 | C17H19FN4O2S |
| CAS号 | 860352-01-8 |
| 稳定性 | ≥ 2 years |
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