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IACS-010759(IACS-10759)

Names

[ CAS No. ]:
1570496-34-2

[ Name ]:
IACS-010759(IACS-10759)

[Synonym ]:
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

Biological Activity

[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


[Related Small Molecules]

Captisol | Cyclosporin A | H2DCFDA | 0MPTP hydrochloride | GW4869 | Etomoxir | TD139 | Mitoquinone mesylate | GSK2795039 | JC-1 | BAPTA-AM | AP 20187 | Setanaxib (GKT137831) | D-Luciferin | Crotaline

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
768.0±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C25H25F3N6O4S

[ Molecular Weight ]:
562.564

[ Flash Point ]:
418.3±35.7 °C

[ Exact Mass ]:
562.161011

[ LogP ]:
3.91

[ Vapour Pressure ]:
0.0±2.6 mmHg at 25°C

[ Index of Refraction ]:
1.648

[ Storage condition ]:
-20℃

Related Compounds