计算溶液所需的质量、体积或浓度。
为什么选择此级别
，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
AG-024322 is a potent ATP-competitive pan- CDK inhibitor against cell cycle kinases CDK1 , CDK2 , and CDK4 with K i values in the 1-3 nM range AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis
In Vitro
AG-024322 (0.1-30 μM; 24 hours) is less toxic at concentrations below 3 µM, the viability of human PBMCs as measured by ATP content with a TC 50 value of 1.4 µM for human PBMCs. AG-024322 (0-120 nM) exhibits growth inhibition effects on HCT-116 cells. It is slightly less potent in the functional cellular assay with an IC 50 of 120 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AG-024322 (intravenous infusion; 2, 6, and 10 mg/kg; 5 days) exhibits no-adverse-effect at 2 mg/kg with mean plasma AUC (0-24.5) of 2.11 g.h/mL. At 6 mg/kg produces pancytic bone marrow hypocellularity, lymphoid depletion. And vascular injury at the injection site renal tubular degeneration occurs at 10 mg/kg . AG-024322 (20 mg/kg) inhibits the growth of established human tumor xenografts of different origins with tumor growth inhibition (TGI) ranging from 32% to 86.4%.It also exhibits anti-tumor effects as a dose-pdependent manner. AG-024322 (20 mg/kg) causes a 65% TGI in the MV522 tumor model. It results a 52% TGI at 1/2 of the maximum tolerated dose (MTD) and only slight anti-tumor activity at 1/4 of the MTD. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male and female cynomolgus monkeys Dosage: 2, 6, and 10 mg/kg (Toxicity analysis) Administration: Intravenous infusion; 5 days Result: Resulted in dose-dependent pancytic bone marrow hypocellularity and lymphoid depletion in lymph nodes, spleen, and/or thymus at >6 mg/kg.
IC50& Target:COX-1 2.3 nM (Ki) COX-2 3 nM (Ki) COX-4 2.9 nM (Ki)
规格
规格或纯度
10mM in DMSO
英文名称
AG-024322
生化机理
AG-024322 是一种针对细胞周期激酶 CDK1、CDK2 和 CDK4 的强效 ATP 竞争性泛 CDK 抑制剂，其 K i 值在 1-3 nM 范围内。AG-024322 具有广谱的抗肿瘤活性和明确的体内靶向调节作用。AG-024322 Ind
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 4 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CCNCC1=CN=CC(=C1C)C2=CC3=C(C=C2)NN=C3C4=NC5=C(N4)C=C(C=C5F)F
关联CAS
PubChem CID
MeSH Entry Terms
AG 024322;AG-024322;AG024322;N-((5-(3-(4,6-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl)-4-methylpyridin-3-yl)methyl)ethanamine
分子量
418.44
技术文档
高级数据
产品属性
| ALogP | 3.7 |
|---|
安全和危险性（GHS）
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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