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MTI-31 (LXI-15029) is a novel low-toxicity mTORC1/mTORC2 inhibitor. MTI-31 demonstrated a potent mTOR binding affinity with >5000 fold selectivity over the related PI3K family isoforms. MTI-31 inhibited mTORC1- and mTORC2 function at ≤120 nM in cellular assays or 5 mg/kg orally in tumor-bearing mice. In a panel of breast cancer lines, the antitumor efficacy of MTI-31 was dependent on HER2+ and/or PIK3CAmut (HER2+/PIK3CAmut) status of the tumors and required mTORC2-specific modulation of Bim, MCL-1 and GSK3. MTI-31 potently inhibited cell proliferation (IC50 <1 μmol/L) and in vivo tumor growth in multiple NSCLC models of EGFR/T790M, EML4-ALK, c-Met, or KRAS (MED <10 mg/kg). In EGFR-mutant and/or EML4-ALK-driven NSCLC, MTI-31 or disruption of mTORC2 reduced cell migration, hematogenous metastasis to the lung, and abrogated morphological and functional traits of EMT. MTI-31 also suppressed programmed death ligand 1 (PD-L1) in EGFR- and ALK-driven NSCLC, mediated in part by mTORC2/AKT/GSK3β-dependent proteasomal degradation.
In vivo, the safety and anti-glioma efficiency of DVAP-liposomes/MTI-31 were validated in intracranial glioma bearing BALB/c nude mice. While showing both systemic and immunological safety, DVAP-liposome/MTI-31 treatment resulted in a significant improvement in the median survival time (24.5 days for saline, 26 days for free MTI-31, 25 days for liposomes/MTI-31 and 36 days for DVAP-liposome/MTI-31). The results highlight MTI-31 as an effective anti-glioma agent when encapsulated in non-immunogenic glioma-targeted liposomes, which may contribute to the development of better anti-glioma treatment.
| Molecular Weight | 474.57 |
| Formula | C26H30N6O3 |
| CAS Number | 1567915-38-1 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related mTOR Products |
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| RMC-4627
RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth. |
| RMC-4529
RMC-4529 has an IC50 value of 1.0 nM against p-4E-BP1-(T37/46) in mTOR kinase cellular assay. |
| WYE-687 dihydrochloride
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. |
| Rapamycin-d3
Rapamycin-d3 |
| L-Leucine-d10
L-Leucine-d10 |
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Products are for research use only. Not for human use. We do not sell to patients.
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