CPI-203
货号：
15479-25mg 基本售价：
7084.0 元 规格：
25 mg
产品信息
概述| 货号 | 15479-25mg |
| 描述 | (+)-JQ1 (Item No. 11187) binds to the acetyl-lysine recognition pocket of bromodomains 1 and 2 on BRD4 with Kd values of ~50 and 90 nM, respectively.1 This displaces BRD4 from nuclear chromatin in cells, inducing differentiation and growth arrest in midline carcinoma cells.1 CPI-203 is a primary amide analog of (+)-JQ1 which has shown superior bioavailability with oral or i.p. administration.2 It is comparable or superior to (+)-JQ1 in inhibiting BRD4 binding and action in vitro or in cells.2,3 CPI-203 arrests the growth of leukemic T cells in vitro(EC50 = 91 nM) and rapidly suppresses leukemia burden in mice.2 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Filippakopoulos, P.,Qi, J.,Picaud, S., et al. Selective inhibition of BET bromodomains. Nature 468(7327), 1067-1073 (2010).
2.King, B.,Trimarchi, T.,Reavie, L., et al. The ubiquitin ligase FBXW7 modulates leukemia-initiating cell activity by regulating MYC stability. Cell 153(7), 1552-1566 (2013).
3.Devaiah, B.N.,Leiw, B.A.,Cherman, N., et al. BRD4 is an atypical kinase that phosphorylates serine 2 of the RNA polymerase II carboxy-terminal domain. Proceedings of the National Academy of Sciences of the United States of America 109(18), 6927-6932 (2012).
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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 | 399.9 |
| 分子式 | C19H18ClN5OS |
| CAS号 | 1446144-04-2 |
| 稳定性 | ≥ 2 years |
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