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编 号:F741515
分子式:C43H45BrCl2N3OP
分子量:801.62
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
Mito-LND (Mito-Lonidamine) is an orally active and mitochondria-targeted inhibitor of oxidative phosphorylation (OXPHOS). Mito-LND inhibits mitochondrial bioenergetics, stimulates the formation of reactive oxygen species, and induces autophagic cell death in lung cancer cells.

体内研究:
Mito-LND (7.5?μmol/kg; oral gavage; 5 days per week; for 3 consecutive weeks) treatment markedly enhanced potency against both lung cancer progression and metastasis. Mito-LND also decreases the rate of growth of A549 tumor xenografts.Mito-LND treatment shows a marked decrease in lung cancer brain metastasis in NOD/SCID mice bearing H2030BrM3 cells.Animal Model:Athymic nude mice (5 weeks) injected with H2030BrM3 cells
Dosage:7.5?μmol/kg
Administration:Oral gavage; 5 days per week; for 3 consecutive weeks
Result:Significantly decreased tumor progression.

体外研究:
Mito-LND blocks lung cancer growth, migration, and invasion. Mito-LND inhibits cell growth of H2030BrM3 and A549 cells with IC50 values of 0.74 μM and 0.69?μM, respectively.Mito-LND inhibits mitochondrial complex I and II activities with IC50 values of 1.2 μM and 2.4?μM, respectively in H2030BrM3 cells. Mito-LND (1?μM) increases ROS generation in H2030BrM3 lung cancer cells. Mito-LND potently induces mitochondrial ROS generation in H2030BrM3 lung cancer cells.Mito-LND (2?μM) decreases the levels of phosphorylated AKT. Mito-LND also decreases the phosphorylation of P70S6K and other energy-sensing proteins in both the parental and metastatic lung cancer cell lines, indicating that Mito-LND specifically downregulates mTOR signaling.
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