ARS853

ARS853 is an inhibitor of K-RAS^G12C, a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells.¹ ARS853 binds to the inactive GDP-bound state of K-RAS^G12C. It decreases the level of active GTP-bound K-RAS by 95% when used at a concentration of 10 µM in K-RAS^G12C mutant lung cancer cells. It also decreases phosphorylation of c-RAF, ERK, and Akt. ARS853 inhibits proliferation of six lung cancer cell lines containing the K-RAS^G12C mutation, including H358 cells (IC₅₀ = 2.5 µM), but does not inhibit proliferation of PC-9 cells, which contain wild-type K-RAS.

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1. Lito, P., Solomon, M., Li, L.-S., et al. Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism. Science 351(6273), 604-608 (2016).