WRX606 is an inhibitor for mTOR complex 1 (mTORC1). WRX606 inhibits the phosphorylation of mTORC1 substrate S6 kinase 1 S6K1 (IC50=10 nM), and the phosphorylation of the eukaryotic translation initiation factor 4E binding protein (p-4E-BP1) (IC50=0.27 μM) in MCF-7. WRX606 exhibits cytotoxicity to HepG2 with IC50 of 17 nM. WRX606 exhibits antitumor efficacy in mouse models.
References:
[1]. Shams R, et al., In Silico and In Cell brid Selection of Nonrapalog Ligands to Allosterically Inhibit the Kinase Activity of mTORC1. J Med Chem. 2022 Jan 27;65(2):1329-1341.