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CO-1686 (AVL-301)EGFR inhibitor

CO-1686 (AVL-301)

Catalog No. A3320
Size Price Stock Qty
10mM (in 1mL DMSO) $60.00 In stock
5mg $50.00 In stock
10mg $80.00 In stock
50mg $165.00 In stock
100mg $255.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

CO-1686

Biological Activity

Description CO-1686 is an irreversible and orally delivered inhibitor of EGFR with IC50 values of 21.5 nM and 303.3 nM for L858R/T790M mutant EGFR and wild-type EGFR, respectively.
Targets L858R/T790M mutant EGFR wild-type EGFR        
IC50 21.5 nM 303.3 nM        

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Chemical Properties

Cas No. 1374640-70-6 SDF Download SDF
Synonyms AVL-301;CNX-419; Rociletinib
Chemical Name N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
Canonical SMILES CC(=O)N1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F)OC
Formula C27H28F3N7O3 M.Wt 555.55
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

CO-1686 is an irreversible and orally delivered inhibitor of mutant EGFR with IC50 value of < 0.51 nM for recombinant EGFR L858R/T790M [1].

CO-1686 covalently modified Cys797 in the ATP binding pocket of the EGFR kinase. It also modified this residue in the EGFR L858R/T790M kinase domain. In the in vitro assay, CO-1686 potently inhibited EGFR L858R/T790M kinase with about 22-fold selectivity over wild-type EGFR. Among the 23 targets treated with CO-1686, EGFR del19, T790M, L858R/T790M and L858R mutants demonstrated the highest inhibition degree. In 4 NSCLC cell lines expressing mutant EGFR (HCC827, PC9, HCC827-EPR and NCI-H1975), CO-1686 potently inhibited cell proliferation with GI50 values of 7-32 nM. CO-1686 also inhibited some minor EGFR mutants including G719S, the exon 19 insertion and L861Q. In mice with NCI-H1975 xenografts, 100 mg/kg/day administration of CO-1686 caused tumor regressions [2].

References:
[1] Walter A O, Tjin R, Haringsma H, et al. CO-1686, an orally available, mutant-selective inhibitor of the epidermal growth factor receptor (EGFR), causes tumor shrinkage in Non-Small Cell Lung Cancer (NSCLC) with T790M resistance mutations. Mol Cancer Ther, 2011, 10(11 Suppl).
[2] Walter A O, Sjin R T T, Haringsma H J. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.