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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-CNX2006
CNX2006

Chemical Structure : CNX2006

CAS No.: 1375465-09-0

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CNX2006 (CNX 2006, CNX-2006)

货号: PC-38035Not For Human Use, Lab Use Only.

CNX2006 (CNX-2006) is a potent, covalent, mutant-selective EGFR inhibitor with IC50 of <20 nM, weak inhibition at wild-type EGFR.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CNX2006 (CNX-2006) is a potent, covalent, mutant-selective EGFR inhibitor with IC50 of <20 nM, weak inhibition at wild-type EGFR.
CNX2006 inhibits the phosphorylation of EGFR-T790M alone or the T790M mutation in cis with activating mutations with IC50 of 46 and 61 nM in NSCLC cell lines NCI-H1975 and PC9GR4, respectively.
CNX-2006 affected the WT-EGFR only at concentrations 10-fold higher than the ones necessary to inhibit mutated receptor.
CNX-2006 is also active against rare EGFR mutations, including EGFR-G719S, -ex19ins (I744-K745insKIPVAI), -L861Q, -ex20ins (H773-V774HVdup), and -T854A.
CNX-2006 inhibits mutant-EGFR cell proliferation by inducing apoptosis in vitro. CNX-2006 inhibits EGFR-T790M tumor growth in vivo.

物理化学性质&存储条件

分子量 545.53
分子式 C26H27F4N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

1. Galvani E, et al. Oncotarget. 2015 Dec 15;6(40):42717-32.

2. Mizuuchi H, et al. Cancer Sci. 2016 Apr;107(4):461-8.

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