CAY10682
货号：
15574-10mg 基本售价：
10640.0 元 规格：
10 mg
产品信息
概述| 货号 | 15574-10mg |
| 描述 | (±)-Nutlin-3 (Item No. 10004372) blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo.1 CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway.2 It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKKɛ (IC50s = 80.5, 78.2, and 57.1 µM, respectively).2 CAY10682 blocks the growth of cancer cells in vitro(IC50s = 2-6 µM) and inhibits the growth of A549 cell xenografts in mice without significantly reducing body weight.2 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Vassilev, L.T.,Vu, B.T.,Graves, B., et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science 303, 844-848 (2004).
2.Zhuang, C.,Miao, Z.,Wu, Y., et al. Double-edged swords as cancer therapeutics: Novel, orally active, small molecules simultaneously inhibit p53-MDM2 interaction and the NF-κB pathway. Journal of Medicinal Chemistry 57(3), 567-577 (2014).
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| 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 | 570.5 |
| 分子式 | C30H25BrFN5O |
| CAS号 | 1542066-74-9 |
| 稳定性 | ≥ 2 years |
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