Name: CO-1686 (AVL-301)
Price: 196.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    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].
    
    [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.
- Properties
  - Alternative Name
    
    AVL-301;CNX-419; Rociletinib; N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
    
    CAS Number
    
    1374640-70-6
    
    Molecular Formula
    
    C27H28F3N7O3
    
    Molecular Weight
    
    555.55
    
    Appearance
    
    A solid
    
    Purity
    
    99.28%
    
    Solubility
    
    ≥27.8 mg/mL in DMSO; insoluble in H2O; ≥4.68 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Cheriyan VT, Alsaab H, et al. "A CARP-1 functional mimetic compound is synergistic with BRAF-targeting in non-small cell lung cancers." Oncotarget. 2018 Jul 3;9(51):29680-29697. PMID:30038713

CO-1686 (AVL-301)

CO-1686 (AVL-301)

Background

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