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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
AT7519, 细胞周期蛋白依赖性激酶抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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.
In vitro
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 Data
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%
规格
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
储存条件
-80℃储存
运输条件
特低温运输
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
名称和识别符
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=
技术文档
高级数据
产品属性
| ALogP | 2.6 |
|---|
关联靶点（人）
CDK1
Tchem
细胞周期蛋白依赖性激酶 1(Cyclin-dependent kinase 1)
(1 活性数据)
CASK
Tchem
外周质膜蛋白CASK(Peripheral plasma membrane protein CASK)
(1 活性数据)
CDK13
Tchem
细胞周期蛋白依赖性激酶 13(Cyclin-dependent kinase 13)
(1 活性数据)
CDK7
Tchem
细胞周期蛋白依赖性激酶 7(Cyclin-dependent kinase 7)
(1 活性数据)
CDK9
Tchem
细胞周期蛋白依赖性激酶9(Cyclin-dependent kinase 9)
(4 活性数据)
CDK16
Tchem
细胞周期蛋白依赖性激酶 16(Cyclin-dependent kinase 16)
(2 活性数据)
CDKL5
Tchem
细胞周期蛋白依赖性激酶类 5(Cyclin-dependent kinase-like 5)
(1 活性数据)
CDK11B
Tchem
细胞周期蛋白依赖性激酶 11B(Cyclin-dependent kinase 11B)
(1 活性数据)
CDK4
Tclin
细胞周期蛋白依赖性激酶4(Cyclin-dependent kinase 4)
(4 活性数据)
CDK18
Tchem
细胞周期蛋白依赖性激酶 18(Cyclin-dependent kinase 18)
(1 活性数据)
CDK14
Tchem
细胞周期蛋白依赖性激酶 14(Cyclin-dependent kinase 14)
(1 活性数据)
CDK11A
Tchem
细胞周期蛋白依赖性激酶 11A(Cyclin-dependent kinase 11A)
(1 活性数据)
CDK17
Tchem
细胞周期蛋白依赖性激酶 17(Cyclin-dependent kinase 17)
(2 活性数据)
CDK2
Tchem
细胞周期蛋白依赖性激酶2(Cyclin-dependent kinase 2)
(2 活性数据)
CDK5
Tchem
细胞周期蛋白依赖性类激酶 5(Cyclin-dependent-like kinase 5)
(2 活性数据)
CILK1
Tchem
丝氨酸/苏氨酸蛋白激酶 ICK(Serine/threonine-protein kinase ICK)
(1 活性数据)
CDK6
Tclin
细胞周期蛋白依赖性激酶 6(Cyclin-dependent kinase 6)
(1 活性数据)
CLK3
Tchem
双特异性蛋白激酶 CLK3(Dual specificity protein kinase CLK3)
(1 活性数据)
GSK3B
Tclin
糖原合酶激酶-3β(Glycogen synthase kinase-3 beta)
(1 活性数据)
GSK3A
Tclin
糖原合酶激酶-3α(Glycogen synthase kinase-3 alpha)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 45 mg/mL (196.3 mM); Ethanol: 45 mg/mL (196.3 mM); Water: Insoluble;
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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