Mito-LND 是一种有口服活性和靶向线粒体的氧化磷酸化抑制剂。它抑制线粒体生物能,刺激活性氧的形成,并诱导肺癌细胞自噬细胞死亡。
产品描述
Mito-LND is an orally active and mitochondria-targeted inhibitor of oxidative phosphorylation.
体外活性
Mito-LND inhibits cell growth of H2030BrM3 and A549 cells with IC50 of 0.74 μM and 0.69?μM, respectively. Mito-LND inhibits mitochondrial complex I and II activities with IC50 of 1.2 μM and 2.4?μM, respectively in H2030BrM3 cells. Mito-LND potently induces mitochondrial ROS generation in H2030BrM3 lung cancer cells. Mito-LND 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.
体内活性
Mito-LNDtreatment 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.
Cas No.
2361564-49-8
分子式
C43H45BrCl2N3OP
分子量
801.63
别名
Mito-Loidamine
储存和溶解度
DMSO:45mg/ml(56.14mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years