IA-Monomer

IA-Monomer (4-[2-(3,4,5,6-tetrahydropyrimidine-2-ylamino)ethyloxy]benzoyl-2-(S)-aminoethylsulfonyl-amino-beta-alanine monomer) is a non-peptide small molecule antagonist of integrin alpha-V beta-3 (αvβ3). Developed by researchers at the Methodist Hospital Research Institute and Weill Medical College of Cornell University, it was designed to target the RGD (Arg-Gly-Asp) motif recognition site on angiogenic endothelial cells. The compound was evaluated as part of a multivalent strategy to enhance anti-tumor efficacy, where it served as the monomeric building block for dimeric and trimeric versions. In preclinical studies using B16F10 melanoma tumor-bearing mice, IA-Monomer demonstrated anti-tumor activity, although it was found to be less effective than its multivalent counterparts (IA-Dimer and IA-Trimer) in reducing tumor volume. Its mechanism involves the selective destruction of tumor vessels by inhibiting αvβ3-mediated interactions without harmful effects on normal microvessels.

Other names

4-[2-(3,4,5,6-tetrahydropyrimidine-2-ylamino)ethyloxy]benzoyl-2-(S)-aminoethylsulfonyl-amino-beta-alanine monomer