计算溶液所需的质量、体积或浓度。
| 活性类型 | Relation | Activity value | Units | Action Type | 期刊 | PubMed Id | doi | Assay Aladdin ID |
|---|
为什么选择此级别
提供 ≥99% 纯度，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
-20°C储存。超低温运输 。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
CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC 50 s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent
In Vitro
CDK5 inhibitor 20-223 (10 nM-10 μM; 72 hours) potently inhibits cell growth in a panel of colorectal cancer (CRC) cell lines. ?\nCDK5 inhibitor 20-223 (0.3125-20 μM; 6 hours) induces a dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels in each of the three CRC cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: CRC cell lines SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells Concentration: 10 μM, 1 μM, 100 nM, 10 nM Incubation Time: 72 hours Result: Reduced cell growth. IC50s of 168±20, 480±41, 360±72, 763±92, 117±49, 568±49, 79±31 nM for SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells. Western Blot AnalysisCell Line: CRC cell lines GEO, HCT116 and HT29 Concentration: 20, 10, 5, 2.5, 1.25, 0.625, 0.3125 μM Incubation Time: 6 hours Result: Did not affect the total levels of CDK2/5, and the levels of total FAK or total Retinoblastoma protein (Rb). Induced a dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels.
In Vivo
CDK5 inhibitor 20-223 (8mg/kg; subcutaneously; for 14 injections) shows anti-tumor activity in human CRC xenograft tumors in nude mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Athymic nude mice Dosage: 8 mg/kg Administration: Injections were given subcutaneously daily for the first week and every other day for two more weeks for a total of 14 injections. Result: Reduced tumor growth and tumor weight in vivo.
Form:Solid
IC50& Target:CDK2 6.0 nM (IC 50 ) CDK5 8.8 nM (IC 50 )
规格
别名
CDK5 抑制剂 20-223
规格或纯度
≥99%
英文名称
CDK5 inhibitor 20-223
生化机理
CDK5 抑制剂 20-223 是一种强效的 CDK2 和 CDK5 抑制剂，其 IC 50 s 分别为 6.0 和 8.8 nM。CDK5 抑制剂 20-223 是一种有效的抗结直肠癌（CRC）药物。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
未知
IUPAC Name
N-(5-cyclobutyl-1H-pyrazol-3-yl)-2-naphthalen-2-ylacetamide
INCHI
1S/C19H19N3O/c23-19(20-18-12-17(21-22-18)15-6-3-7-15)11-13-8-9-14-4-1-2-5-16(14)10-13/h1-2,4-5,8-10,12,15H,3,6-7,11H2,(H2,20,21,22,23)
InChi Key
AGVIDDQHAQSPIZ-UHFFFAOYSA-N
Smiles
C1CC(C1)C2=CC(=NN2)NC(=O)CC3=CC4=CC=CC=C4C=C3
Isomeric SMILES
C1CC(C1)C2=CC(=NN2)NC(=O)CC3=CC4=CC=CC=C4C=C3
PubChem CID
分子量
305.37
技术文档
高级数据
三维结构
交互式化学结构模型
关联靶点（人）
BXPC-3
(2997 活性数据)
MIA PaCa-2
(5949 活性数据)
ASPC1
(1310 活性数据)
CDK5
Tchem
Cyclin-dependent kinase 5/CDK5 activator 1
(3697 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
溶解性
DMSO : 100 mg/mL (327.47 mM; Need ultrasonic)
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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