IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research In Vitro IACS-010759 hydrochloride (10, 30, 100 nM; for 4 or 5 days) reduces viability and induces apoptosis in primary AML. IACS-010759 hydrochloride (0.001, 0.01, 0.1, 1, 10, 100, 1000 nM; 72 hurs) robustly inhibits both OCR and galactose-dependent H460 cell viability and has nearly identical IC50 values of 1.4 nM. IACS-010759 hydrochlorideis similarly active in mouse (average IC50 = 5.6 nM), rat (IC50 = 12.2 nM), and cynomolgus monkey (IC50 = 8.7 nM) cell lines. IACS-010759 hydrochloride (0.01-10 μM) yieldes a maximal reduction of growth of > 50% in the majority of cancer cell lines (24 of 30 pancreatic (PDAC), 19 of 20 ovarian, 13 of 16 triple-negative breast (TNBC), 8 of 10 non-small-cell lung (NSCLC)) and a subset (11of 30 PDAC, 10 of 20 ovarian, 5 of 16 TNBC, 2 of 10 NSCLC) exhibited > 100% growth inhibition. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo IACS-010759 hydrochloride (5, 10, 25 mg/kg/day; oral; for 21 d) results in tumor regression with minimal body weight loss at the 5 or 10 mg/kg dose in mice bearing NB-1 (PGD-) subcutaneous xenografts. IACS-010759 at the 25 mg/kg dose is not tolerated . IACS-010759 HCl (10 mg/kg; orally; QD (daily) or QD×5 (5 d on/2 d off); for 35 d) increases median survival from 28 d to longer than 60 d, whereas less-frequent dosing schedules (Q2D or Q3D) enhances survival to a lesser extent . IACS-010759 hydrochloride (0.3 mg/kg for iv; 1 mg/kg for oral) has low plasma clearance with a high volume of distribution, resulting in a prolonged terminal half-life (>24 h) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:OXPHOS
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IACS-010759 hydrochloride
CAS number：1807523-99-4 molecular formula：C25H26ClF3N6O4S
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| Chinese alias | IACS-010759 盐酸盐 | ||
| English alias | XZ543NW1NF | HY-112037A | IACS-10759 HCl | IACS-010759 hydrochloride | MS-30604 | 1807523-99-4 | 1807523-99-4 (HCl) | 5-[5-methyl-1-[[3-(4-methylsulfonylpiperidin-1-yl)phenyl]methyl]-1,2,4-triazol-3-yl]-3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazole;hydr | ||
| CAS number | 1807523-99-4 | molecular formula | C25H26ClF3N6O4S |
| molecular weight | 562.563646 g/mol | Exact mass | ≥99% |
| PSA | 125.000 Ų | logp | - |
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