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IACS-010759
- IACS-10759
Axon 2909
CAS:
1570496-34-2
Purity:
99%
- Soluble in DMSO
- MF: C25H25F3N6O4S
- MW: 562.56
Description
IACS-010759 is an orally bioavailable, potent inhibitor of complex I of oxidative phosphorylation (OXPHOS). IACS-010759 was active in mouse, rat and cynomolgus monkey with IC50 values of 5.6 nM, 12.2 nM and 8.7 nM, respectively. Treatment with IACS-010759 robustly inhibited proliferation and induced apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS, likely owing to a combination of energy depletion and reduced aspartate production that leads to impaired nucleotide biosynthesis.
More Information
| Parent CAS No. | 1570496-34-2 |
|---|---|
| Chemical Name | 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 |
| SMILES | C1(N2CCC(S(=O)(=O)C)CC2)C=C(CN2N=C(C3ON=C(C4C=CC(OC(F)(F)F)=CC=4)N=3)N=C2C)C=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C25H25F3N6O4S/c1-16-29-23(24-30-22(32-38-24)18-6-8-20(9-7-18)37-25(26,27)28)31-34(16)15-17-4-3-5-19(14-17)33-12-10-21(11-13-33)39(2,35)36/h3-9,14,21H,10-13,15H2,1-2H3 |
| InChiKey | HWJWNWZJUYCGKV-UHFFFAOYSA-N |
| CID | 86711931 |
| Short Description | OxPhos inhibitor |
References
- M Protopopova et al. Abstract 4380: IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities. Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015.
- JR Molina et al. An inhibitor of oxidative phosphorylation exploits cancer vulnerability. Nat Med. 2018 Jul;24(7):1036-1046.
- HV Vangapandu et al. Biological and metabolic effects of IACS-010759, an OxPhos inhibitor, on chronic lymphocytic leukemia cells. Oncotarget. 2018 May 18;9(38):24980-24991.
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