CO-1686

Description

CO-1686 is an irreversible kinase inhibitor that specifically targets mutant forms of the epidermal growth factor receptor (EGFR) including T790M (K_i = 21.5 nM) with significantly reduced activity at the wild-type form of the receptor (K_i = 303.3 nM). CO-1686 has been shown to inhibit the proliferation of non-small cell lung cancer (NSCLC) cells expressing mutant EGFR with GI₅₀ values ranging from 7-32 nM in vitro, inducing apoptosis. It also demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft and transgenic models dosed orally at 100 mg/kg/day.

The Uses of CO-1686

CO 1686 is seen as an irreversible epidermal growth factor receptor (EFGR1) kinase inhibitor.

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.