| Cas No.: | 1570496-34-2 |
| Chemical Name: | IACS-010759 free base |
| Synonyms: | 5-(5-methyl-1-(3-(4-(methylsulfonyl)piperidin-1-yl)benzyl)-1H-1,2,4-triazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole;IACS-10759 (IACS-010759 );IACS-010759;HWJWNWZJUYCGKV-UHFFFAOYSA-N;IACS 010759 - Bio-X;BCP20596;s8731;AK549747;4-Methanesulfonyl-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;5-[5-Methyl-1-[[3-(4-methylsulfonylpiperidin-1-yl)phenyl]methyl]-1,2,4-triazol-3-yl]-3-[4-(trifluoro |
| SMILES: | S(C([H])([H])[H])(C1([H])C([H])([H])C([H])([H])N(C2=C([H])C([H])=C([H])C(C([H])([H])N3C(C([H])([H])[H])=NC(C4=NC(C5C([H])=C([H])C(=C([H])C=5[H])OC(F)(F)F)=NO4)=N3)=C2[H])C([H])([H])C1([H])[H])(=O)=O |
| Formula: | C25H25F3N6O4S |
| M.Wt: | 562.568 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS). |
| 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]. |
| In Vitro: | IACS-10759 inhibits the conversion of NADH to NAD+ in an immunoprecipitated complex I assay at low nM concentrations[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 |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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