ARS-853 (ARS853) is a mutant-specific, covalent inhibitor of KRAS G12C with IC50 of 2.5 uM.
ARS-853 engages KRASG12C in biochemical assay with a rate constant of 76 M-1s-1, > 600-fold improvement compared with Compound 12 (Ostrem JM, Nature 2013;503:548–51.).
ARS-853 inhibits growth of H358 cells.
ARS-853 is the first direct KRAS inhibitor shown to selectively inhibit KRAS in cells with potency in the range of a drug candidate.
