上海莼试生物技术有限公司
上海莼试生物技术有限公司
| 规格 | 5mg 10mg 25mg 50mg 100mg 200mg 500mg |
| CAS | 1807523-99-4 |
| 别名 | N/A |
| 化学名 | N/A |
| 分子式 | C25H26ClF3N6O4S |
| 分子量 | 599.02 |
| 溶解度 | DMSO: ≥ 100 mg/mL (166.94 mM); H2O: < 0.1 mg/mL (insoluble) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述：
IACS-10759 Hydrochloride is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS). OXPHOS[1]
IACS-10759 inhibits the conversion of NADH to NAD+ in an immunoprecipitated complex I assay at low nM concentrations[1].
IACS-10759 is orally bioavailable with excellent physicochemical properties in preclinical species and achieves significant in vivo efficacy with daily oral dosing of 10-25 mg/kg. There is a >50 day extension of median survival in an orthotopic AML cell line xenograft and robust regression in DLBCL and GBM xenograft models[1].
[1]. Protopopova M. IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 4380. doi:10.1158/1538-7445.AM2015-4380
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