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IACS-010759 hydrochloride

🥰Excellent
Catalog No. T27568Cas No. 1807523-99-4
Alias IACS-10759 hydrochloride, IACS10759 hydrochloride, IACS-010759 HCl, IACS010759 HCl

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.

IACS-010759 hydrochloride

IACS-010759 hydrochloride

🥰Excellent
Purity: 98.81%
Catalog No. T27568Alias IACS-10759 hydrochloride, IACS10759 hydrochloride, IACS-010759 HCl, IACS010759 HClCas No. 1807523-99-4
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 SizePriceAvailabilityQuantity
2 mg$68In Stock
5 mg$122In Stock
1 mL x 10 mM (in DMSO)$162In Stock
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Purity:98.81%
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Product Introduction

Bioactivity
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].
AliasIACS-10759 hydrochloride, IACS10759 hydrochloride, IACS-010759 HCl, IACS010759 HCl
Chemical Properties
Molecular Weight599.03
FormulaC25H26ClF3N6O4S
Cas No.1807523-99-4
SmilesCl.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 & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM1.6694 mL8.3468 mL16.6937 mL83.4683 mL
5 mM0.3339 mL1.6694 mL3.3387 mL16.6937 mL
10 mM0.1669 mL0.8347 mL1.6694 mL8.3468 mL
20 mM0.0835 mL0.4173 mL0.8347 mL4.1734 mL
50 mM0.0334 mL0.1669 mL0.3339 mL1.6694 mL

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