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HP661是一种针对线粒体复合物I(也称为NADH脱氢酶)的抑制剂,对复合物I具有选择性,以1 µM的浓度抑制其77.6%,而对复合物III抑制率为28.1%,对复合物II和IV则无抑制作用。HP661特异性降低具有高水平氧化磷酸化作用的人类肺癌细胞H460、NCI H441及对trametinib耐药的A549细胞的生存能力(IC50分别为10.6、29.7和15.1 nM),相较于氧化磷酸化水平低的NCI H358人类肺癌细胞(IC50 >10,000 nM)以及非癌性人类胰腺正常上皮细胞(HPNE)和MRC-5人类胎肺成纤维细胞(两者的IC50均>10,000 nM)。当以每天两次,每次30 mg/kg的剂量给药时,HP661在H460小鼠异种移植模型中减少肿瘤体积,并对trametinib引导的肿瘤生长减少产生加成效应。
HP661是一种针对线粒体复合物I(也称为NADH脱氢酶)的抑制剂,对复合物I具有选择性,以1 µM的浓度抑制其77.6%,而对复合物III抑制率为28.1%,对复合物II和IV则无抑制作用。HP661特异性降低具有高水平氧化磷酸化作用的人类肺癌细胞H460、NCI H441及对trametinib耐药的A549细胞的生存能力(IC50分别为10.6、29.7和15.1 nM),相较于氧化磷酸化水平低的NCI H358人类肺癌细胞(IC50 >10,000 nM)以及非癌性人类胰腺正常上皮细胞(HPNE)和MRC-5人类胎肺成纤维细胞(两者的IC50均>10,000 nM)。当以每天两次,每次30 mg/kg的剂量给药时,HP661在H460小鼠异种移植模型中减少肿瘤体积,并对trametinib引导的肿瘤生长减少产生加成效应。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,960 | 35日内发货 | |
5 mg | ¥ 8,270 | 35日内发货 |
产品描述 | HP661, a selective inhibitor of mitochondrial complex I (NADH dehydrogenase), impedes complex I activity by 77.6% at 1 µM, demonstrating lesser inhibition towards complex III (28.1%) and no inhibitory effects on complexes II and IV. It notably decreases the viability of human lung cancer cells—H460, NCI H441, and trametinib-resistant A549 cells (IC50s = 10.6, 29.7, and 15.1 nM, respectively)—which exhibit high levels of oxidative phosphorylation. In contrast, it shows minimal activity against NCI H358 lung cancer cells and non-cancerous HPNE and MRC-5 cells (IC50s = >10,000 nM for both), which have lower oxidative phosphorylation levels. Furthermore, in an H460 mouse xenograft model, HP661 at a dose of 30 mg/kg twice daily significantly reduces tumor volume and enhances the tumor-growth inhibitory effects of trametinib. |
分子量 | 661.60 |
分子式 | C31H29F6N7O3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | Methanol: Soluble Ethanol: Soluble Chloroform: Soluble |
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