| Name | CNX-2006 |
| Description | CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR. |
| 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) |
| Kinase Assay | Growth inhibition assays: Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays. |
| Animal Research | Animal Models: Nude miceFormulation: 5% DMSO:15% Solutol HS15 in PBSDosages: 25 mg/kgAdministration: i.p. |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMF : soluble
DMSO : 91 mg/mL (166.81 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | HER1 | ErbB-1 | Epidermal growth factor receptor | EGFR (mutant) | EGFR | CNX-2006 |
| Inhibitors Related | (S)-Afatinib | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Erlotinib hydrochloride | Erlotinib | Neratinib | Afatinib | Chalcone | Brigatinib | Genistein | Gefitinib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Anti-Colorectal Cancer Compound Library | Apoptosis Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | JAK-STAT Compound Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max |
United States
