BIM-26226

BIM-26226 is a **potent and selective antagonist of the gastrin-releasing peptide receptor (GRPR)** and bombesin receptor, with an IC50 of 6 nM for GRPR. It inhibits BN- or GRP-stimulated amylase release in vitro and suppresses the growth of experimental pancreatic acinar carcinoma in vivo. BIM-26226 was investigated as an anticancer agent, particularly for its ability to inhibit growth of GRP-stimulated tumors, but development was discontinued in Phase 1. The compound is a synthetic peptide originally developed by Ipsen and is primarily of interest for research into cancer therapeutics targeting peptide G-protein coupled receptors[1][2][3][4][7][9].

Other names

D-Pentafluorophenylalanyl-L-glutaminyl-L-tryptophyl-L-alanyl-L-valyl-D-alanyl-L-histidyl-L-leucine methyl ester(D-Pentafluorophenylalanyl6,D-alanyl11)bombesin (6-13) methyl ester{D-F5 Phe}-Gln-Trp-{D-Ala}-Val-Ala-His-Leu-OMeL-Leucine, 2,3,4,5,6-pentafluoro-D-phenylalanyl-L-glutaminyl-L-tryptophyl-L-alanyl-L-valyl-D-alanyl-L-histidyl-, methyl ester