biostudies-literatureUnknown1(9)Jin MThis report describes the investigation of a series of 5,7-disubstituted imidazo[5,1-f][1,2,4]triazine inhibitors of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR). Structure-activity relationship exploration and optimization leading to the identification, characterization, and pharmacological activity of compound 9b, a potent, selective, well-tolerated, and orally bioavailable dual inhibitor of IGF-1R and IR with in vivo efficacy in tumor xenograft models, is discussed.ACS medicinal chemistry letters510-5https://www.ebi.ac.uk/biostudies/studies/S-EPMC4007908biostudies-literatureDiscovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR.PMC4007908Laufer RSKleinberg ACooke AGokhale PCMulvihill MJStolz KMForeman KWerner DSLandfair DFeng LSiu KWYao YWild RBittner MALi AHDong HJin MSteinig AGKadalbajoo MMay EWBuck EPachter JAfalseDiscovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR.This report describes the investigation of a series of 5,7-disubstituted imidazo[5,1-f][1,2,4]triazine inhibitors of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR). Structure-activity relationship exploration and optimization leading to the identification, characterization, and pharmacological activity of compound 9b, a potent, selective, well-tolerated, and orally bioavailable dual inhibitor of IGF-1R and IR with in vivo efficacy in tumor xenograft models, is discussed.2010-01-01T00:00:00Z2010 Dec2025-04-05T10:37:36.761Z2019-03-27T01:27:30ZS-EPMC40079082490024010.1021/ml100178g