| Name | IACS-010759 hydrochloride |
| Description | IACS-010759 hydrochloride is an orally potent and selective OXPHOS inhibitor that inhibits proliferation and induces apoptosis in OXPHOS-dependent brain cancer and acute myeloid leukaemia models for the study of relapsed/refractory AML and advanced solid tumours. |
| In vitro | IACS-010759 hydrochloride shows potent in vitro activity by reducing AML cell viability and inducing apoptosis at concentrations of 10-100 nM over 4-5 days. It also inhibits mitochondrial OCR and oxidative phosphorylation-dependent viability in H460 cells, with an average IC₅₀ of 1.4 nM over 72 h. Similar potency was observed in cells from mice (IC₅₀ = 5.6 nM), rats (12.2 nM), and cynomolgus monkeys (8.7 nM)[1]. |
| In vivo | In NB-1 neuroblastoma xenograft mice, oral IACS-010759 hydrochloride at 5-10 mg/kg for 21 days significantly reduced tumor size, although 25 mg/kg was not well tolerated. In another model, daily or alternate-day dosing at 10 mg/kg for 35 days extended survival from 28 to over 60 days, and lower-frequency dosing (e.g., 2×/week) also improved outcomes. Pharmacokinetic studies showed that a 0.3 mg/kg dose had low clearance, limited distribution, and a prolonged half-life (>24 h)[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (83.47 mM), Sonication is recommended.
2% DMSO+40% PEG300+5% Tween 80+53% Saline : 1 mg/mL (1.67 mM), Suspension.
H2O : < 1 mg/mL (insoluble)
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| Keywords | IACS-10759 | IACS10759 | IACS-010759 Hydrochloride | IACS010759 hydrochloride | IACS-010759 | IACS010759 | IACS 10759 | IACS 010759 hydrochloride | IACS 010759 |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Bioactive Compound Library | Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
