AG61

AG61 is a small molecule microtubule-targeting agent (MTA) belonging to the tricyclic thieno[2,3-d]pyrimidine class. Developed through a collaboration between Duquesne University and the University of Texas Health Science Center at San Antonio, AG61 was designed to overcome common drug resistance mechanisms, such as P-glycoprotein (Pgp) efflux and βIII-tubulin expression, which often limit the clinical efficacy of taxanes and vinca alkaloids. The compound exerts its antitumor effects by binding to the colchicine site on tubulin, leading to microtubule depolymerization and subsequent cell cycle arrest. In preclinical evaluations, AG61 demonstrated nanomolar antiproliferative potency against human melanoma cell lines (MDA-MB-435) and potent microtubule-disrupting activity.

Other names

2-amino-N4-methoxyphenyl tricyclic thieno[2,3-d]pyrimidine