IACS-010759

IACS-010759 is an orally bioavailable small molecule inhibitor of mitochondrial complex I (NADH ubiquinone oxidoreductase), a key component of the electron transport chain involved in oxidative phosphorylation (OxPhos)[1][3][6][8]. By binding to and inhibiting complex I at the ubiquinone-binding site, it disrupts energy production in tumor cells that rely on OxPhos for survival and proliferation[6][8]. This leads to energy depletion, impaired nucleotide biosynthesis, autophagy induction, inhibition of cell proliferation, and ultimately tumor cell death[6][8]. Developed by MD Anderson Cancer Center[6], IACS‑010759 is under clinical investigation for relapsed/refractory acute myeloid leukemia (AML), solid tumors, and lymphoma. It shows particular promise against cancers with reduced glycolytic capacity or resistance to other therapies such as Bruton’s tyrosine kinase inhibitors[6].

Other names

1570496-34-25-(5-methyl-1-(3-(4-(methylsulfonyl)piperidin-1-yl)benzyl)-1H-1,2,4-triazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazoleIACS-010759 free baseIACS010759 free baseIACS 010759 free base