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- 爱必信(absin)
- 上海
- abs815999
- 2026年10月19日
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- 文献和实验
- 技术资料
- 保存条件：
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
- 保质期：
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
- 英文名：
-
- 库存：
99
- 供应商：
爱必信(上海)生物科技有限公司
- CAS号：
602306-29-6
- 规格：
50mg/10mg/5mg
| 规格： | 50mg | 产品价格： | ￥4545.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥1320.0 |
| 规格： | 5mg | 产品价格： | ￥849.0 |
| 公告提醒：爱必信所有产品和服务仅用于科学研究，不用于临床应用及其他用途提供产品和服务（也不为任何个人提供产品和服务）!
抑制剂描述： 产品名称：AZD5438 产品别名：见爱必信官网 英文别名：AZD5438 靶点：CDK CAS：602306-29-6 纯度：99% 外观：见爱必信官网 保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. 描述： AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It is less potent to CDK5/6 and also inhibits GSK3β. Phase 1. 溶解性：体外: 体外研究： AZD5438 potently inhibits the kinase activity of cyclin E-cdk2, cyclin A-cdk2, cyclin B1-cdk1, p25-cdk5, cyclin D3-cdk6, and cyclin T-cdk9 (IC50, 6, 45, 16, 21, and 20 nM, respectively). AZD5438 potently inhibits the kinase activity of cyclin E-cdk2, cyclin A-cdk2, cyclin B1-cdk1, p25-cdk5, cyclin D3-cdk6, and cyclin T-cdk9 (IC50, 6, 45, 16, 21, and 20 nM, respectively). In common with many other cdk inhibitors, AZD5438 also inhibits the kinase activity of p25-cdk5 and glycogen synthase kinase 3β in vitro (IC50, 14 and 17 nM, respectively). AZD5438 significantly augments cellular radiosensitivity in NSCLC cells. Combined treatment with AZD5438 and irradiation also enhances tumor growth delay, with an enhancement factor ranging from 1.2-1.7. 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.
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文献和实验与SLC7A11之间并非直接的底物传递，而是通过GLS1间接偶联——ASCT2提供谷氨酰胺，GLS1转化为谷氨酸，SLC7A11再利用谷氨酸换取胱氨酸。同时靶向SLC1A5和SLC7A11可能协同破坏肿瘤细胞的抗氧化防线。SLC1A5抑制剂V-9302在临床前模型中显示出抗肿瘤活性，但临床转化尚处于早期。 MCT与乳酸代谢 SLC16家族的单羧酸转运蛋白MCT1和MCT4介导乳酸跨膜转运，维持肿瘤微环境酸碱平衡。MCT1抑制剂AZD3965是首--个进入临床试验的SLC16家族靶向
Characterization of the Picrotoxin Site of GABAA Receptors
. 2012. AZD‐3043: A novel, metabolically labile sedative‐hypnotic agent with rapid and predictable emergence from hypnosis. Anesthesiology 116:1267‐1277. Elliott, K.A.C
