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Product name : CNX-2006
Item : CR1778
Price : 100mg, $745; 200mg, $1185
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Additional Information :  We offer significant discount for bulky quantity order,Please ask price and availability of other quantities
CAS : 1375465-09-0
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Details:
 Chemical Information
M.Wt 545.53 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C26H27F4N7O2
CAS No 1375465-09-0
Solubility

DMSO 100mg/ml; Water <1 mg/ml



Biological Activity of 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.
IC50 value: <20 nM
Target: Mutant EGFR
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. CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model.

 

[1]. Kadoaki Ohashi, et al. CNX-2006, a Novel Irreversible Epidermal Growth Factor Receptor (EGFR) Inhibitor, Selectively Inhibits EGFR T790M and Fails to Induce T790M-Mediated Resistance In Vitro

[2]. Elena Galvani, et al. Role of epithelial-mesenchymal transition (EMT) in sensitivity to CNX- 2006,a novel mutant-selective EGFR inhibitor which overcomes in vitro T790M-mediated resistance in NSCLC


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