1570496-34-2

1570496-34-2 structure

Name: IACS-010759(IACS-10759)
Chemical Name: 4-(Methylsulfonyl)-1-{3-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-1,2,4-triazol-1-yl)methyl]phenyl}piperidine
CAS Number: 1570496-34-2
Molecular Formula: C₂₅H₂₅F₃N₆O₄S
Molecular Weight: 562.564
Catalog: Research Areas Cancer
Create Date: 2018-06-07 13:23:22
Modify Date: 2024-01-01 20:06:34
IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).

Name	4-(Methylsulfonyl)-1-{3-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-1,2,4-triazol-1-yl)methyl]phenyl}piperidine
Synonyms	4-(Methylsulfonyl)-1-{3-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-1,2,4-triazol-1-yl)methyl]phenyl}piperidine Piperidine, 4-(methylsulfonyl)-1-[3-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-1,2,4-triazol-1-yl]methyl]phenyl]- IACS-10759

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