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K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRASG12C[1].

K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRASG12C[1]. K-Ras G12C-IN-4 (4 hours) exhibits IC50=0.219 μM for inhibition of MAPK signaling (p-ERK) in MIA PaCa-2 cells[1].K-Ras G12C-IN-4 (72 hours) translates to a 0.067 μM IC50 for inhibition of cellular viability in a CellTiter-Glo experiment in MIA PaCa-2 cells[1].

[1]. Shin Y, et al. Discovery of N-(1-Acryloylazetidin-3-yl)-2-(1H-indol-1-yl)acetamides as Covalent Inhibitors of KRASG12C. ACS Med Chem Lett. 2019 Aug 20;10(9):1302-1308.