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AT7519
| 品牌 | 厂商性质 | 产地 | 货期 |
|---|---|---|---|
| 阿拉丁 | 生产商 | 上海 | 现货 |
产品参数
| 货号 | CAS号 | 操作 |
|---|---|---|
| A127001-100mg | 844442-38-2 | 询价 |
| A127001-25mg | 844442-38-2 | 询价 |
| A127001-5mg | 844442-38-2 | 询价 |
产品介绍
属性
| 溶解性 | Soluble in DMSO (10 mg/ml) at 25°C, water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25°C. |
| 存贮条件 | 储存温度-20°C |
描述
| 应用 | A novel small molecule effective as a pan-Cdk inhibitor for Cdk1, Cdk2, Cdk3, Cdk4, Cdk5 and Cdk6. |
| 产品介绍 | AT7519是多种CDK抑制剂，作用于CDK1， 2， 4， 6和9时，IC50为10-210 nM，对CDK3作用效果稍弱，对CDK7几乎没有抑制活性。Phase 2。 |
| 备注 | AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. Phase 1. |
| 生化机理 | AT7519 is a novel small molecule effective as a multi-cyclin-dependent kinase inhibitor for Cdk1/cyclin B (IC50 = 210 nM), Cdk2/Cyclin A (IC50 = 47 nM), Cdk3/Cyclin E (IC50 = 360 nM), Cdk4/Cyclin D1 (IC50 = 100 nM), Cdk5/p35 (IC50 = 13 nM) and Cdk6/Cyclin D3 (IC50 = 170 nM). AT7519 is an ATP competitive Cdk inhibitor with a Ki value of 38 nM for Cdk1. AT7519 is inactive against all non-Cdk kinases with the exception of GSK3β (IC50 = 89 nM). AT7519 shows potent antiproliferative activity in a variety of human tumor cell lines with IC50 values ranging from 40 nM for MCF-7 to 940 nM for SW620. AT7519 induces activation of GSK-3β by down-regulating GSK-3β phosphorylation, which also contributes to AT7519 induced apoptosis independent of the inhibition of transcription. |
| 别名 | N-(4-哌啶基)-4-(2,6-二氯苯甲酰氨基)-1H-吡唑-3-甲酰胺;AT 7519;AT-7519;4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide;N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide |
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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途