MTI-31

MTI-31 (LXI-15029, mTOR inhibitor-31) is a novel potent, selective mTORC1/mTORC2 inhibitor with Kd of 0.2 nM (mTOR), displays >5,000-fold selectivity over PIK3CA, PIK3CB and PIK3G; showed an IC50 value 39 nM in LANCE® assay of mTOR substrate phosphorylation; dose-dependently inhibits of both the mTORC1 substrates P-S6K1(T389), P-S6(S235/6), P-4EBP1(T70) and mTORC2 substrate P-AKT(S473) tumor cell lines harboring mTOR pathway dysregulation with IC50 of <0.12 uM; potently inhibited cell proliferation (IC50 <1 mmol/L) and in vivo tumor growth in multiple NSCLC models of EGFR/T790M, EML4-ALK, c-Met or KRAS (MED <10 mg/kg), also suppressed programmed death ligand 1 (PD-L1) in EGFR- and ALK-driven NSCLC, mediated in part by mTORC2/AKT/GSK3β-dependent proteasomal degradation.

References 1. Qian J, et al. Oncotarget. 2016 Oct 11;7(41):67071-67086. 2. Zhang Q, et al. Clin Cancer Res. 2019 Feb 22. pii: clincanres.2548.2018. View Related Products by Target mTOR