NVP-AEW541

Description: NVP-AEW541 (also known as AEW541; AEW-541) is a novel, potent and selective inhibitor of IGF-1R/InsR with potential antineoplastic activity. It inhibits IGF-1R/InsR with IC50s of 150 nM/140 nM in cell-free assays. NVP-AEW541 has greater potency and selectivity for IGF-1R in a cell-based assay. NVP- AEW541 abrogates IGF-I-mediated survival and colony formation in soft agar at concentrations that are consistent with inhibition of IGF-IR autophosphorylation. In vivo, this orally bioavailable compound inhibits IGF-IR signaling in tumor xenografts and significantly reduces the growth of IGF-IR-driven fibrosarcomas. Thus, NVP- AEW541 represents a class of selective, small molecule IGF-IR kinase inhibitors with proven in vivo antitumor activity and potential therapeutic application.