您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > CNX-2006
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
CNX-2006
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CNX-2006图片
CAS NO:1375465-09-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议

产品介绍
CNX-2006 是一种突变选择性和不可逆的 EGFR 抑制剂,对 EGFRT790M 的 IC50 低于 20 nM。
Cas No.1375465-09-0
化学名N-(3-((2-((4-((1-(2-fluoroethyl)azetidin-3-yl)amino)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide
Canonical SMILESFC(F)(F)C1=C(NC2=CC(NC(C=C)=O)=CC=C2)N=C(NC3=CC=C(NC4CN(CCF)C4)C=C3OC)N=C1
分子式C26H27F4N7O2
分子量545.53
溶解度≥ 27.3mg/mL in DMSO
储存条件Store at -20° C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

CNX-2006, a structural analog of CO-1686, is a selective and irreversible inhibitor of mutant-EGFR with IC50 value of < 20 nM.

The epidermal growth factor receptor (EGFR) is the cell-surface receptor for epidermal growth factor and plays an important role in tumor invasion and cancer cell proliferation.

CNX-2006 is a novel and irreversible mutant-selective EGFR inhibitor with very weak inhibition of wild-type EGFR. In non-small cell lung cancer (NSCLC) models expressing mutant EGFR-T790M, CNX-2006 inhibited EGFR signaling. CNX-2006 acquired resistance which was drove by NF-κB. So NF-κB activation might replace the EGFR signaling. These results suggested that inhibition of NF-κB pathway was a promising therapy method for patients who progressed after treatment with mutant-selective EGFR inhibitors [1].

Reference:
[1].Galvani E, Sun J, Leon LG, et al. NF-κB drives acquired resistance to a novel mutant-selective EGFR inhibitor. Oncotarget, 2015.