| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S80827-5mg |
98% | ￥400.00 |
4 | - | - | - | - |
|
S80827-10mg |
98% | ￥600.00 |
2 | - | - | - | - |
|
S80827-50mg |
98% | ￥2200.00 |
1 | - | - | - | - |
|
S80827-100mg |
98% | ￥4000.00 |
1 | - | - | - | - |
|
| 产品描述： | AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC50s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6 | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | cdk2-cyclin E:6 nM (IC50);cdk2-cyclin A:45 nM (IC50);cdk5-p25:14 nM (IC50);cdk1-cyclin B1:16 nM (IC50);cdk9-cyclin T:20 nM (IC50);cdk6-cyclin D3:21 nM (IC50);cdk4-cyclin D1:449 nM (IC50);cdk7-cyclin H:821 nM (IC50);CDK | ||||||||||||||||||||
| 体内研究： | AZD5438 (50 mg/kg twice daily or 75 mg/kg, p.o.) inhibits human tumor xenograft growth. In vivo, AZD5438 reduces the proportion of actively cycling cells. Further pharmacodynamic analysis of AZD5438-treated SW620 xenografts shows that efficacious doses of AZD5438 (>40% tumor growth inhibition) maintains suppression of biomarkers, such as phospho-pRbSer249/Thr252, for up to 16 hours following a single oral dose | ||||||||||||||||||||
| 参考文献： | 1. Byth KF, et al. AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. Mol Cancer Ther. 2009 Jul;8(7):1856-66. Epub 2009 Jun 9. 2. Raghavan P, et al. AZD5438, an Inhibitor of Cdk1, 2, and 9, Enhances the Radiosensitivity of Non-Small Cell Lung Carcinoma Cells. Int J Radiat Oncol Biol Phys. 2012 Jul 12. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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