Shopping Cart
- Remove All
- Your shopping cart is currently empty
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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $68 | In Stock | |
5 mg | $122 | In Stock | |
1 mL x 10 mM (in DMSO) | $162 | In Stock |
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. |
Targets&IC50 | Mitochondrial oxidative phosphorylation (Rat primary cells):12.2 nM, Mitochondrial oxidative phosphorylation (Mouse primary cells):5.6 nM, Mitochondrial oxidative phosphorylation (Cynomolgus monkey primary cells):8.7 nM, Mitochondrial oxidative phosphorylation (AML patient-derived cells):10-100 nM (4-5 days), Mitochondrial oxidative phosphorylation (H460 cells):1.4 nM (72 h) |
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]. |
Alias | IACS-10759 hydrochloride, IACS10759 hydrochloride, IACS-010759 HCl, IACS010759 HCl |
Molecular Weight | 599.03 |
Formula | C25H26ClF3N6O4S |
Cas No. | 1807523-99-4 |
Smiles | Cl.O=S(=O)(C)C1CCN(C2=CC=CC(=C2)CN3N=C(N=C3C)C4=NC(=NO4)C=5C=CC(OC(F)(F)F)=CC5)CC1 |
Relative Density. | no data available |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (83.47 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
|
Copyright © 2015-2025 TargetMol Chemicals Inc. All Rights Reserved.