Co-1686


Catalog No. size PriceQuantity
M111-2S 2 mg solid $79
M111-10S 10mg solid $320

Description

Product Information
Molecular Weight: 555.55
Formula: C27H28F3N7O3
Purity: >98%
CAS#: 1374640-70-6
Solubility: DMSO: ≥ 43 mg/mL
Chemical Name: N-(3-((2-((4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide
Storage: Powder -20oC 3 years 4oC 2 years In solvent -80oC 6 months -20oC 1 month

 

Biological Activity:


CO-1686 is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

How to use:

In Vitro: CO-1686 (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. CO-1686 potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. CO-1686 resistant NSCLC cell lines are sensitive to AKT inhibition[1].

In Vivo: CO-1686 (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. CO-1686 (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice[1].

Reference:

[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25.

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