PD318088

CAS: 391210-00-7 货号: P408043 分子式: C16H13BrF3IN2O4 分子量: 561.1
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
P408043-1ml
现货 Stock Image
¥1,429.90
请输入您要添加的产品数量
🧪
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

PD318088是ATP非竞争性MEK1/2变构抑制剂,能与ATP同时结合于MEK1,且其结合位点与ATP结合位点相邻。A small molecule inhibitor of MEK-1 and MEK-2

Information

PD318088 is a non-ATP competitive allostericMEK1/2inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
In vitro

PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure.

In vivo


Cell Data

cell lines:HUVEC

Concentrations:

Incubation Time:

Powder Purity:≥99%

规格

英文别名
5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)benzamide
规格或纯度
10mM in DMSO
英文名称
PD318088
生化机理
PD318088 是一种非 ATP 竞争性异构 MEK1/2 抑制剂,与 ATP 同时结合在 MEK1 活性位点的一个区域,该区域毗邻 ATP 结合位点。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C1=CC(=C(C=C1I)F)NC2=C(C(=C(C=C2C(=O)NOCC(CO)O)Br)F)F
分子量
561.1
Reaxy-Rn
13493289
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=13493289&ln=

技术文档

📋 安全数据表 (SDS)

全面的危险、操作、储存及法规合规文件。

下载 SDS →

✅ 分析证书 (COA)

批次质量数据。输入批号以获取对应 COA。

查询 COA →

📊 产品数据表

产品规格和应用的快速参考摘要。

查看数据表 →

🔬 规格说明书

该级别的完整质量属性和验收标准。

查看规格说明 →

高级数据

化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 48 mg/mL (196.51 mM); Ethanol: 48 mg/mL (196.51 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