化合物CNX2006 T6008

Product Introduction
Bioactivity


英文名: CNX-2006

描述: CNX-2006 是一种新型的不可逆突变选择性 EGFR 抑制剂，对 EGFRT790M 的IC50值小于 20 nM。

细胞实验: 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.(Only for Reference)

激酶实验: Growth inhibition assays: Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays.

动物实验: Animal Models: Nude miceFormulation: 5% DMSO:15% Solutol HS15 in PBSDosages: 25 mg/kgAdministration: i.p.

体外活性: 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. [1]CNX-2006 resistent cells shows increased expression of EMT markers and MMP9.[2]

体内活性: CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model. [1] [2]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMF : soluble
DMSO : 91 mg/mL(166.8 mM)


关键字: CNX-2006 | HER1 | inhibit | Epidermal growth factor receptor | ErbB-1 | Inhibitor | EGFR

相关产品: WS3 | Lapatinib | Withanolide A | Cetuximab | DZD1516 | CP-724714 | Ginsenoside Rh2 | CGP77675 | Sanguinarine chloride | Almonertinib mesylate

相关库: Cysteine Covalent Library | Anti-Prostate Cancer Compound Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Highly Selective Inhibitor Library | Target-Focused Phenotypic Screening Library

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