VS-5095

VS-5095 is a potent, selective, and orally active small molecule inhibitor of focal adhesion kinase (FAK, also known as PTK2). Developed by Verastem, VS-5095 targets the ATP-binding site within the FAK kinase domain, blocking fibronectin-stimulated FAK autophosphorylation at Tyr397 with low nanomolar cellular potency. By inhibiting FAK, VS-5095 disrupts integrin-mediated signaling pathways that regulate cell adhesion, migration, survival, and epithelial-to-mesenchymal transition (EMT). Preclinical studies have demonstrated that VS-5095 attenuates breast cancer stem cell self-renewal and inhibits tumor growth and metastasis in vivo, particularly in triple-negative breast cancer (TNBC) models.