| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A408650-1ml |
1ml |
现货  |
|
| 英文别名 | 4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | AT7519 |
| 生化机理 | AT7519 是 CDK1、2、4、6 和 9 的多重 CDK 抑制剂，IC50 为 10-210 nM。它对 CDK3 的抑制作用较弱，对 CDK7 的活性较低。AT7519 还能抑制 GSK3β，IC50 为 89 nM。AT7519 可诱导细胞凋亡。第二阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 细胞周期蛋白依赖性激酶抑制剂 |
| 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。A novel small molecule effective as a pan-Cdk inhibitor for Cdk1, Cdk2, Cdk3, Cdk4, Cdk5 and Cdk6. Information AT7519 is a multi-CDKinhibitor for CDK1, 2, 4, 6 and 9 withIC50of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also inhibitsGSK3βwith IC50 of 89 nM. AT7519 inducesapoptosis. Phase 2. 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 consistent with the inhibition of CDK1 and CDK2. AT7519 induces dose-dependent cytotoxicity in multiple myeloma (MM) cell lines with IC50 values ranging from 0.5 to 2 μM at 48 hours, with the most sensitive cell lines being MM.1S (0.5 μM) and U266 (0.5 μM) and the most resistant MM.1R (>2 μM). It does not induce cytotoxicity in peripheral blood mononuclear cells (PBMNC). AT7519 partially overcomes the proliferative advantage conferred by IL6 and IGF-1 as well as the protective effect of bone marrow stromal cells (BMSCs). AT7519 induces rapid dephosphorylation of RNA pol II CTD at serine 2 and serine 5 sites, and leads to the inhibition of transcription, partially contributing to AT7519 induced cytotoxicity of MM cells. 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. In vivo A twice daily dosing of AT7519 (9.1 mg/kg) causes tumor regression of both early-stage and advanced-stage s.c. tumors in the HCT116 and HT29 colon cancer xenograft models. AT7519 treatment (15 mg/kg) inhibits tumor growth and prolongs the median overall survival of mice in the human MM xenograft mouse model in association with increased caspase 3 activation. cell lines： Concentrations：Dissolved in DMSO at a concentration of 10 mM, final concentrations 0.25-4 μM Incubation Time：24 or 48 hours Powder Purity:≥99% |
| ALogP | 2.6 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C1CNCCC1NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl |
| 分子量 | 382.24 |
| Reaxy-Rn | 28045917 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=28045917&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 45 mg/mL (196.3 mM); Ethanol: 45 mg/mL (196.3 mM); Water: Insoluble; |
|---|
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