IACS-10759 Hydrochloride (Synonyms: IACS-10759 hydrochloride) |
Catalog No.GC36286 |
IACS-10759 염산염은 산화적 인산화(OXPHOS) 억제제의 경구 활성, 강력한 미토콘드리아 복합체 I입니다. IACS-10759 염산염은 OXPHOS에 의존하는 뇌암 및 급성 골수성 백혈병(AML) 모델에서 증식을 억제하고 세포자멸사를 유도합니다. IACS-10759 염산염은 재발성/불응성 AML 및 고형 종양 연구의 가능성이 있습니다.
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Cas No.: 1807523-99-4
Sample solution is provided at 25 µL, 10mM.
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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