Information IACS-010759 (IACS-10759) IACS-010759 (IACS-10759) is a potent and selective oxidative phosphorylation inhibitor (IC50 Targets oxidative phosphorylation 10 nM In vitro IACS-010759 significantly reduced viability measured by CTG assay in all cell lines tested (Notch mutant: Pf382, 1301, Jurkat, MOLT-4, P12-Ichikawa and Notch wt: T-ALL1). Treatment of T-ALL with IACS-010759 had effectively inhibited FA-stimulated mitochondrial respiration indicated by decreased oxygen consumption rates (OCR). However, the cells maintain an ability to generate energy via glycolysis, indicated by high extracellular acidification rate (ECAR) in both, control and IACS-treated groups. In CLL cells, IACS-010759 causes minimal cell death, inhibits oxygen consumption rate (OCR) and increases glycolysis. It also decreases intracellular ribonucleotide triphosphate pools in CLL. In sensitive AML cells IACS-010759 induces AMPK activation leading to mTOR suppression which results in cell growth inhibition in AML cells. AMPK and mTOR could be putative biomarkers of anti-leukemia activity of the novel OxPhosi IACS-010759. Cell Research(from reference) Cell lines：CLL cells Concentrations：30 nM, 100 nM, 300 nM, 1 μM, and 3 μM Incubation Time：24 or 48 h
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IACS-010759 (IACS-10759)
Dangerous GoodsCAS number：1570496-34-2 molecular formula：C25H25F3N6O4S
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | AKOS030527987 | 1570496-34-2 | A936426 | Oxidative phosphorylation inhibitor IACS-010759 | HY-112037 | NSC809972 | NSC-809972 | IACS-010759 free base | 4-Methanesulfonyl-1-{3-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-1,2,4-tria | ||
| CAS number | 1570496-34-2 | molecular formula | C25H25F3N6O4S |
| molecular weight | 562.56 g/mol | Exact mass | ≥99% |
| PSA | 125.000 Ų | logp | 4.800 |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
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