化合物MTI-31 T35343

Product Introduction
Bioactivity


英文名: MTI-31

描述: MTI-31 (LXI-15029) 是口服有效的，高度选择性的mTORC1和mTORC2抑制剂，对 mTOR 的Kd 为 0.20 nM，IC50为 39 nM。MTI-31可用于乳腺癌的研究。

体外活性: 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].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 8.33 mg/mL (17.55 mM)


关键字: mTOR kinase inhibitor | tissue factor | LXI 15029 | mTORC2 | mTOR inhibitor | Inhibitor | EGFR mutant cancer | mTOR-TF axis | Mammalian target of Rapamycin | MTI31 | apoptosis | mTOR | inhibit | MTI 31 | mTORC1 | lipid metabolism | LXI15029 | tumor microenvironment

相关产品: mTOR inhibitor-1 | Salidroside | mTOR inhibitor-11 | mTOR inhibitor 9e | JR-AB2-011 | Ridaforolimus | ElteN378 | Rapamycin | LY 303511 | mTOR inhibitor-8

相关库: Antioxidant Compound Library | Anti-Cancer Metabolism Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Active Compound Library | Metabolism Compound Library | Anti-Pancreatic Cancer Compound Library | Glycolysis Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途