INT2-31

INT2-31 (also known as C31) is a novel small molecule inhibitor designed to specifically disrupt the protein-protein interaction (PPI) between Focal Adhesion Kinase (FAK) and the Insulin-like Growth Factor 1 Receptor (IGF-1R). This interaction is critical for cell survival signaling in various aggressive malignancies, including pancreatic cancer, esophageal cancer, and melanoma. By targeting this specific scaffold-mediated interaction, INT2-31 inhibits downstream survival signaling pathways, notably reducing the phosphorylation of Akt and ERK1/ERK2. Preclinical studies have demonstrated that INT2-31 significantly inhibits tumor cell proliferation and induces apoptosis both as a monotherapy and in synergistic combination with chemotherapeutic agents like 5-fluorouracil (5-FU). It was identified through high-throughput screening and has shown efficacy in reducing tumor growth in multiple in vivo xenograft models.