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CNX-2006

EGFR/ErbB1 选择性抑制剂 | 活化剂
规格或纯度: 10mM in DMSO
有货

库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
C421426-1ml
1ml 现货 Stock Image

基本描述

英文别名 2-Propenamide,N-[3-[[2-[[4-[[1-(2-fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-
规格或纯度 10mM in DMSO
英文名称 CNX-2006
生化机理 CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
储存温度 -80℃储存
运输条件 超低温冰袋运输
产品介绍


Information

CNX-2006 is a novel irreversible mutant-selectiveEGFRinhibitor withIC50of < 20 nM, with very weak inhibition at wild-type EGFR.

Targets

mutant EGFR <20 nM

In vitro

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.

In vivo

CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model.

Cell Research(from reference)

Cell lines:HEK293 

Concentrations:~1000 nM 

Incubation Time:6 h 

产品属性

IC50 mutant EGFR, IC50: <20 nM
ALogP 5.15
HBD Count 4
Rotatable Bond 12

名称和标识符

IUPAC Name N-[3-[[2-[4-[[1-(2-fluoroethyl)azetidin-3-yl]amino]-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
INCHI 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)
InChi Key BFSRTTWIPACGMI-UHFFFAOYSA-N
Canonical SMILES COC1=C(C=CC(=C1)NC2CN(C2)CCF)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F
Isomeric SMILES COC1=C(C=CC(=C1)NC2CN(C2)CCF)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F
PubChem CID 56968072
分子量 545.53

化学和物理性质

DMSO(mg / mL) Max Solubility 100
DMSO(mM) Max Solubility 183.3079757
Water(mg / mL) Max Solubility <1

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