BI2865

BI2865 is a potent, non-covalent, small-molecule pan-KRAS inhibitor developed by Boehringer Ingelheim. It is designed to inhibit a broad spectrum of KRAS variants, including wild-type KRAS and major oncogenic mutants such as G12C, G12D, G12V, G13D, and Q61H, by binding to the switch II pocket. Unlike allele-specific inhibitors (e.g., G12C inhibitors), BI2865 acts as a "pan-inhibitor," blocking the interaction of KRAS with its downstream effectors regardless of the specific mutation. In preclinical studies, it has demonstrated the ability to sensitize ovarian cancer cells to chemotherapy (like paclitaxel and cisplatin) and inhibit tumor growth in various KRAS-driven models. It is frequently utilized as a high-quality chemical probe to study KRAS biology and therapeutic potential.