AZD 5363
货号：
15406-1mg 基本售价：
630.0 元 规格：
1 mg
产品信息
概述| 货号 | 15406-1mg |
| 描述 | Akt functions as a key component in multiple signaling pathways including those related to cell proliferation, metabolism, and survival as well as angiogenesis. AZD 5363 is a pyrrolopyrimidine-derived compound that inhibits Akt by competitively binding to the kinase domain, preventing substrate phosphorylation by Akt.1 It inhibits Akt1, 2, and 3 with IC50 values of 3, 7, and 7 nM, respectively and also inhibits P70S6K and PKA with similar potency (IC50s = 6 and 7 nM, respectively).1 Furthermore, AZD 5363 shows >75% inhibition at 1 μM against ROCK-II, MKK1, MSK1, MSK2, PKCγ, PKGα, PKGβ, PRKX, RSK2, and RSK3.1 At 3 μM or less, AZD 5363 has been reported to inhibit the proliferation of 41 out of 182 solid and hematologic tumor cell lines, demonstrating the greatest sensitivity towards breast cancer derived-cells or those with PIK3CA and/or PTEN mutations.1 Oral dosing to nude mice bearing BT474c xenografts resulted in antitumor activity, including the reduction of the phosphorylation of PRAS40, GSK3β, and S6 at an EC50 value of ~ 0.1 μM.1 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Davies, B.R.,Greenwood, H.,Dudley, P., et al. Preclinical pharmacology of AZD5363, an inhibitor of AKT: Pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. Molecular Cancer Therapeutics 11(4), 73-887 (2012).
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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 | 428.9 |
| 分子式 | C21H25ClN6O2 |
| CAS号 | 1143532-39-1 |
| 稳定性 | ≥ 2 years |
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