AIG01012

AIG01012 is a novel, potent small molecule inhibitor of Son of Sevenless homolog 1 (SOS1) developed by AIGEN Sciences. Discovered using the human-in-the-loop (HITL) AI-based platform AIGEN ChemTailor in conjunction with fragment-based drug discovery (FBDD) and molecular modeling, AIG01012 is designed to target pan-KRAS mutant cancers. It works by disrupting the interaction between SOS1 and various KRAS isoforms, including wild-type KRAS and mutants such as G12C, G12D, G12V, and G13D, thereby preventing the exchange of GDP for GTP and inhibiting downstream KRAS signaling. Preclinical data demonstrate significant antiproliferative activity across multiple KRAS-driven cell lines (e.g., H358, MIA-PaCa2, AsPC-1) and synergistic effects when combined with sotorasib, trametinib, or osimertinib. The compound has shown favorable pharmacological properties and efficacy in mouse tumor models, supporting its potential progression into clinical trials.