IACS-10759 Hydrochloride (Synonyms: IACS-10759 hydrochloride) |
| カタログ番号GC36286 |
IACS-10759 塩酸塩は、経口で活性な強力なミトコンドリア複合体 I の酸化的リン酸化 (OXPHOS) 阻害剤です。 IACS-10759 塩酸塩は、OXPHOS に依存する脳腫瘍および急性骨髄性白血病 (AML) のモデルにおいて、増殖を阻害し、アポトーシスを誘導します。 IACS-10759 塩酸塩は、再発/難治性 AML および固形腫瘍の研究の可能性を秘めています。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1807523-99-4
Sample solution is provided at 25 µL, 10mM.
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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
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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