1807523-99-4

1807523-99-4 structure

Name: IACS-10759 Hydrochloride
Chemical Name: IACS-10759 Hydrochloride
CAS Number: 1807523-99-4
Molecular Formula: C₂₅H₂₆ClF₃N₆O₄S
Molecular Weight: 599.02
Catalog: Research Areas Cancer
Create Date: 2019-01-20 18:58:38
Modify Date: 2024-01-03 20:59:52
IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).

Name	IACS-10759 Hydrochloride

Description	IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Cancer
Target	OXPHOS[1]
In Vitro	IACS-10759 inhibits the conversion of NADH to NAD+ in an immunoprecipitated complex I assay at low nM concentrations[1].
In Vivo	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].
References	[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