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位置: 首页> 品牌> Sigma-Aldrich> PIM-Kinase Inhibitor X, CX-6258-Calbiochem

PIM-Kinase Inhibitor X, CX-6258-Calbiochem

品牌
Sigma-Aldrich
货号
526529
规格纯度
The PIM-Kinase Inhibitor X, CX-6258 controls the biological activity of PIM-Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
价格
3352.28 *本价格含增值税费
促销
服务
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  • 包邮
  • 增值税票
数量
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半岛bd体育手机客户端 名称:
PIM-Kinase Inhibitor X, CX-6258-Calbiochem
( E)-5-Chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one, HCl
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

一般描述

An orally bioavailable oxindolo-furanyl compound that acts as a potent, reversible and ATP-competitive inhibitor of pan PIM-kinases (IC50= 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3, respectively; Ki= 5 nM for PIM-1) with excellent selectivity over 107 kinases (IC80>500 nM). Shown to arrest the proliferation of several human cancer cells (IC50= 20 and 452 nM for MV-4-11 and PC3 cells) and block phosphorylation of Bad-Ser112, 4E-BP1-Ser65and Thr37/46with an IC50of ~ 1.0 ?M. Displays favorable pharmacokinetic profile and efficacy in mice, and suppresses tumor growth in MV-4-11 and PC3 xenograft murine model (50 mg/kg, p.o.). Further, potentiates doxorubicin (Cat. No. 324380) and paclitaxel (Cat. No. 580555) toxicity in PC3 cells.

包装

10 mg in Glass bottle
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Primary Target
PIM Kimases
Target IC50: 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3
Reversible: yes
Secondary Target
Flt3

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

其他说明

Haddach, M., et al. 2012.ACS Med. Chem. Lett.3,135.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式 C26H24ClN3O3· xHCl
分子量 461.94 (free base basis)

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥99% (HPLC)
形式 powder
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
desiccated (hygroscopic)
protect from light
颜色 orange
溶解性 DMSO: 25 mg/mL
运输 ambient
储存温度 2-8℃
SMILES string O=C(/C1=C/C2=CC=C(C3=CC=CC(C(N4CCCN(C)CC4)=O)=C3)O2)NC5=C1C=C(Cl)C=C5.[xHCl]

安全信息

储存分类代码 11 - Combustible Solids
WGK WGK 3
闪点(F) Not applicable
闪点(C) Not applicable

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