CPV-337

CPV-337 is a small molecule inhibitor designed to target the interaction between Rac GTPases and the guanine nucleotide exchange factor (GEF) Ect2 (Epithelial Cell Transforming 2). As a derivative of the dual Rac/Cdc42 inhibitor MBQ-167, CPV-337 demonstrates enhanced specificity for Rac isoforms (Rac1, Rac2, Rac3, and Rac1b) and improved potency, with IC50 values in the nanomolar range. By inhibiting Ect2-mediated Rac activation, CPV-337 disrupts downstream signaling through effectors such as PAK, Cofilin, and WAVE, leading to the inhibition of lamellipodia formation, cell migration, and invasion. Preclinical evidence in mouse models of HER2-positive breast cancer and pancreatic cancer indicates that CPV-337 significantly reduces tumor growth and metastatic progression.