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CO-1686(AVL-301)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CO-1686(AVL-301)图片
CAS NO:1374640-70-6
规格:98%
分子量:555.55
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
EGFR inhibitor
CAS:1374640-70-6
分子式:C27H28F3N7O3
分子量:555.55
纯度:98%
存储:Store at -20°C

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].


参考文献:
[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.