Uses
MTI-31 (LXI-15029) is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (Kd: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding assays. MTI-31 shows an IC50 of 39 nM for mTOR in LANCE assay of mTOR substrate phosphorylation with 100 μM ATP. MTI-31 can be used for the research of breast cancer[1].
IC 50
mTOR: 0.2 nM (Ki); mTOR: 39 nM (IC
50, 100 μM ATP); mTORC1; mTORC2
References
[1] Zhang Q, et, al. A Novel mTORC1/2 Inhibitor (MTI-31) Inhibits Tumor Growth, Epithelial-Mesenchymal Transition, Metastases, and Improves Antitumor Immunity in Preclinical Models of Lung Cancer. Clin Cancer Res. 2019 Jun 15;25(12):3630-3642. DOI:
10.1158/1078-0432.CCR-18-2548[2] Qian J, et, al. Molecular regulation of apoptotic machinery and lipid metabolism by mTORC1/mTORC2 dual inhibitors in preclinical models of HER2+/PIK3CAmut breast cancer. Oncotarget. 2016 Oct 11;7(41):67071-67086. DOI:
10.18632/oncotarget.11490[3] Wang X, et, al. Non-immunogenic, low-toxicity and effective glioma targeting MTI-31 liposomes . J Control Release. 2019 Dec 28;316:381-392. DOI:
10.1016/j.jconrel.2019.11.005