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CNX-2006

🥰Excellent
Catalog No. T6008Cas No. 1375465-09-0
Alias CNX2006, CNX 2006

CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.

CNX-2006

CNX-2006

🥰Excellent
Purity: 99.16%
Catalog No. T6008Alias CNX2006, CNX 2006Cas No. 1375465-09-0
CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
Pack SizePriceAvailabilityQuantity
1 mg$34In Stock
2 mg$48In Stock
5 mg$76In Stock
10 mg$128In Stock
25 mg$235In Stock
50 mg$425In Stock
1 mL x 10 mM (in DMSO)$92In Stock
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Purity:99.16%
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Product Introduction

Bioactivity
Description
CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
Targets&IC50
EGFR (mutant):<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. [1]CNX-2006 resistent cells shows increased expression of EMT markers and MMP9.[2]
In vivo
CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model. [1] [2]
Kinase Assay
Growth inhibition assays: Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays.
Cell Research
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)
Animal Research
Animal Models: Nude miceFormulation: 5% DMSO:15% Solutol HS15 in PBSDosages: 25 mg/kgAdministration: i.p.
AliasCNX2006, CNX 2006
Chemical Properties
Molecular Weight545.53
FormulaC26H27F4N7O2
Cas No.1375465-09-0
SmilesCOc1cc(NC2CN(CCF)C2)ccc1Nc1ncc(c(Nc2cccc(NC(=O)C=C)c2)n1)C(F)(F)F
Relative Density.1.396 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMF: soluble
DMSO: 91 mg/mL (166.8 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8331 mL9.1654 mL18.3308 mL91.6540 mL
5 mM0.3666 mL1.8331 mL3.6662 mL18.3308 mL
10 mM0.1833 mL0.9165 mL1.8331 mL9.1654 mL
20 mM0.0917 mL0.4583 mL0.9165 mL4.5827 mL
50 mM0.0367 mL0.1833 mL0.3666 mL1.8331 mL
100 mM0.0183 mL0.0917 mL0.1833 mL0.9165 mL

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