HEC211909

HEC211909 is an orally bioavailable, highly potent small molecule pan-KRAS inhibitor developed by Sunshine Lake Pharma. It targets multiple KRAS mutations, including G12D, G12C, G12V, Q61H, and G13D, as well as KRAS wild-type amplifications. Uniquely, it inhibits both the active (GTP-bound) and inactive (GDP-bound) states of the KRAS protein, functioning as a pan-KRAS ON/OFF inhibitor. Preclinical studies demonstrate significant anti-tumor activity and tumor regression in various KRAS-mutant xenograft models, including colorectal, lung, and pancreatic cancer models. The compound shows high selectivity for KRAS over HRAS and NRAS, which is expected to provide an expanded therapeutic index and good tolerability in normal tissues.