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MTI-31 (LXI-15029) is a potent, orally active, and highly selective inhibitor of mTORC1 and mTORC2, exhibiting a Kd of 0.20 nM for mTOR and >5,000-fold selectivity over PIK3CA, PIK3CB, and PIK3G in binding assays, with an IC50 of 39 nM for mTOR in a LANCE assay of mTOR substrate phosphorylation with 100 μM ATP [1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $197 | In Stock | |
5 mg | $455 | In Stock | |
10 mg | $695 | In Stock | |
25 mg | $1,090 | In Stock | |
50 mg | $1,560 | In Stock | |
100 mg | $2,180 | In Stock |
Description | MTI-31 (LXI-15029) is a potent, orally active, and highly selective inhibitor of mTORC1 and mTORC2, exhibiting a Kd of 0.20 nM for mTOR and >5,000-fold selectivity over PIK3CA, PIK3CB, and PIK3G in binding assays, with an IC50 of 39 nM for mTOR in a LANCE assay of mTOR substrate phosphorylation with 100 μM ATP [1]. |
Targets&IC50 | mTOR:0.2 nM(Kd) |
In vitro | MTI-31 (0.01-100 μM) elicits a potent and more substantial inhibition of cell growth than that of Rapamycin[1]. Treatment with MTI-31 for 6 h demonstrates a dose-dependent inhibition of both the mTORC1 substrates P-S6K1(T389), P-S6(S235/6), P-4EBP1(T70) and mTORC2 substrate P-AKT(S473), achieving 50% inhibition at ≤0.12 μM in three representative tumor cell lines harboring mTOR pathway dysregulation (786-O renal, U87MG glioma and MDA-MB-453 breast)[1]. MTI-31-induced apoptosis requires mTORC2-regulated Bim- and GSK3 activity[1]. |
In vivo | MTI-31(5-40 mg/kg; orally) is efficacious in several tumor models harboring HER2+/PIK3CAmut and/or PTEN-deficiency exemplified by MDA-MB-453 and 786-O[1]. Treatment of tumor bearing nude mice with orally administered MTI-31 inhibits growth of H1975 tumors (25 mg/kg/d; orally) or U87MG tumors (30 mg/kg/d; orally)[2]. |
Alias | MTI-31, LXI-15029 |
Molecular Weight | 474.55 |
Formula | C26H30N6O3 |
Cas No. | 1567915-38-1 |
Smiles | CNC(=O)c1cccc(c1)-c1ccc2c(nc(nc2n1)N1CCOC[C@@H]1C)N1C2CCC1COC2 |
Relative Density. | 1.275 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 8.33 mg/mL (17.55 mM), Sonication and heating to 60℃ are recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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