[CAS NO. 1375465-09-0] CNX-2006
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PRODUCTS SPECIFICATIONS [1375465-09-0]
Store
Catalog
SLK-S7206
Brand
Selleck
CAS
1375465-09-0
DESCRIPTION [1375465-09-0]
Overview
| MDL | MFCD26142654 |
|---|---|
| Molecular Weight | 545.53 |
| Molecular Formula | C26H27F4N7O2 |
| SMILES | C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(NC4CN(CCF)C4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8331 mL | 9.1654 mL | 18.3308 mL |
| 5 mM | 0.3666 mL | 1.8331 mL | 3.6662 mL |
| 10 mM | 0.1833 mL | 0.9165 mL | 1.8331 mL |
| 50 mM | 0.0367 mL | 0.1833 mL | 0.3666 mL |
Description
CNX-2006 is a novel irreversible mutant-selective inhibitor with of < 20 nM, with very weak inhibition at wild-type EGFR.
Targets
| mutant EGFR [1] |
| <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. CNX-2006 resistent cells shows increased expression of EMT markers and MMP9.
In vivo
CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model.
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