IACS-010759(IACS-10759)

Modify Date: 2024-01-01 20:06:34

IACS-010759(IACS-10759) Structure
IACS-010759(IACS-10759) structure
Common Name IACS-010759(IACS-10759)
CAS Number 1570496-34-2 Molecular Weight 562.564
Density 1.5±0.1 g/cm3 Boiling Point 768.0±70.0 °C at 760 mmHg
Molecular Formula C25H25F3N6O4S Melting Point N/A
MSDS N/A Flash Point 418.3±35.7 °C

 Use of IACS-010759(IACS-10759)


IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).

 Names

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
Synonym More Synonyms

 IACS-010759(IACS-10759) Biological Activity

Description IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).
Related Catalog
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

 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℃

 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
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Price: ¥2723/10 mM * 1 mL in DMSO

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