CO-1686 Inhibitor CAS No. 1374640-70-6

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Chemical Characteristic

Product Name	CO-1686
CAS No.	1374640-70-6
Molecular Weight	555.55
Formula	C₂₇H₂₈F₃N₇O₃
Chemical Name	N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
Smiles	C(=O)(C=C)Nc1cc(ccc1)Nc1nc(ncc1C(F)(F)F)Nc1c(cc(cc1)N1CCN(CC1)C(=O)C)OC
Chemical Structure

Biological activities

CO-1686 is a potent and mutant-selective EGFR inhibitor. CO-1686 inhibits EGFRL858R/T790M protein with an IC50 less than 0.51 nM. CO-1686 inhibits cell proliferation of cell lines (H1975 and HCC827) expressing mutant EGFR with GI50s of 48 and 14 nM, respectively. CO-1686 also inhibits EGFR signaling (pAKT, pS6rp, and pMAPK) in H1975 tumors. CO-1686 causes dose-dependent inhibition of pEGFR in tumor tissue in the H1975 NSCLC xenograft model. Oral administration of CO-1686 (3-100 mg/kg) significantly suppresses tumor growth of H1975 cells (L858R/T790M) in a dose-dependent manner, causing tumor regressions at the highest dose (100 mg/kg) without affecting body weight.^[1]

References

[1] Walter AO, 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, 2011.

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