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CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $34 | In Stock | |
2 mg | $48 | In Stock | |
5 mg | $76 | In Stock | |
10 mg | $128 | In Stock | |
25 mg | $235 | In Stock | |
50 mg | $425 | In Stock | |
1 mL x 10 mM (in DMSO) | $92 | In Stock |
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. |
Alias | CNX2006, CNX 2006 |
Molecular Weight | 545.53 |
Formula | C26H27F4N7O2 |
Cas No. | 1375465-09-0 |
Smiles | COc1cc(NC2CN(CCF)C2)ccc1Nc1ncc(c(Nc2cccc(NC(=O)C=C)c2)n1)C(F)(F)F |
Relative Density. | 1.396 g/cm3 (Predicted) |
Storage | Powder: -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
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