compound introduction
ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1. In Vitro KRAS G12C is recently identified to be potentially druggable by allele-specific covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II pocket (S-IIP). Success of this approach requires active cycling of KRAS G12C between its active-GTP and inactive-GDP conformations as accessibility of the S-IIP is restricted only to the GDP-bound state. This strategy proves feasible for inhibiting mutant KRAS in vitro. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:KRAS(G12C)
