GLPBio

IACS-10759 Hydrochloride

Catalog No.: GC36286Purity:>99.50%Synonyms: IACS-10759 hydrochloride
IACS-10759 Hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-10759 Hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-10759 Hydrochloride has the potential for relapsed/refractory AML and solid tumors research.

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IACS-10759 Hydrochloride
Cas No.: 1807523-99-4
10mM (in 1mL DMSO)In Stock
$142.00
1
5mgIn Stock
$108.00
1
10mgIn Stock
$180.00
1
25mgIn Stock
$360.00
1
50mgIn Stock
$585.00
1

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Description

IACS-10759 Hydrochloride is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS). OXPHOS[1]

IACS-10759 inhibits the conversion of NADH to NAD+ in an immunoprecipitated complex I assay at low nM concentrations[1].

IACS-10759 is orally bioavailable with excellent physicochemical properties in preclinical species and achieves significant in vivo efficacy with daily oral dosing of 10-25 mg/kg. There is a >50 day extension of median survival in an orthotopic AML cell line xenograft and robust regression in DLBCL and GBM xenograft models[1].

[1]. Protopopova M. IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 4380. doi:10.1158/1538-7445.AM2015-4380

Product Documents

Purity:>99.50%Appearance:A solid

Chemical Properties

CAS No.
1807523-99-4
Synonyms
IACS-10759 hydrochloride
SMILES
FC(F)(F)OC1=CC=C(C2=NOC(C3=NN(CC4=CC(N5CCC(S(=O)(C)=O)CC5)=CC=C4)C(C)=N3)=N2)C=C1.Cl
Molecular Formula
C25H26ClF3N6O4S
Molecular Weight
599.02
Solubility
DMSO: ≥ 100 mg/mL (166.94 mM); Water: < 0.1 mg/mL (insoluble)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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