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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
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)545.53
FormulaC26H27F4N7O2
CAS No.1375465-09-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (183.3 mM)
Water: <1 mg/mL
Ethanol: 29 mg/mL (53.1 mM)
Other info

Chemical Name: N-(3-((2-((4-((1-(2-fluoroethyl)azetidin-3-yl)amino)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide

InChi Key: BFSRTTWIPACGMI-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H27F4N7O2/c1-3-23(38)33-16-5-4-6-17(11-16)34-24-20(26(28,29)30)13-31-25(36-24)35-21-8-7-18(12-22(21)39-2)32-19-14-37(15-19)10-9-27/h3-8,11-13,19,32H,1,9-10,14-15H2,2H3,(H,33,38)(H2,31,34,35,36)

SMILES Code: C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(NC4CN(CCF)C4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O

Synonyms

CNX-2006; CNX 2006; CNX2006.

实验参考方法
In Vitro

In vitro activity: CNX-2006 is a novel irreversible EGFR tyrosine kinase inhibitor, specifically inhibits activating mutations of EGFR as well as the T790M mutation while having very weak inhibition at wild-type EGFR. In in vitro modeling of acquired resistance, continuous CNX-2006 treatment on drug-sensitive EGFR mutant cells leads to resistance more slowly than erlotinib. Dose escalation with CNX-2006 leads to differential effects in different lines, but does not select for T790M-mediated resistance. CNX-2006 resistent cells shows increased expression of EMT markers and MMP9.


Kinase Assay: Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays.


Cell Assay: Cells with endogenous or transiently transfected mutant EGFRs (293 cells) are treated with inhibitors for 6 hours and then corresponding lysates are extracted and analyzed by immunoblotting.

In VivoCNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model.
Animal modelNude mice
Formulation & Dosage5% DMSO:15% Solutol HS15 in PBS; 25 mg/kg; i.p.
ReferencesGalvani E, Sun J, Leon LG, et al. Oncotarget, 2015.