IACS-10759 Hydrochloride 是氧化磷酸化 (OXPHOS) 复合物I的有效抑制剂。
CAS：1807523-99-4
分子式：C25H26ClF3N6O4S
分子量：599.02
纯度：98%
存储：Store at -20°C

Background:

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