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產(chǎn)品名稱

IACS-010759 - IACS-10759

產(chǎn)品貨號

Axon 2909 CAS [1570496-34-2] MF C25H25F3N6O4SMW 562.56 Purity: 99% Soluble in DMSO Description IACS-010759 is an orally bioavailable, potent inhibitor of complex I of oxidative phosphorylation (OXPHOS). IACS-010759 was active in mouse, rat and cynomolgus monkey with IC50 values of 5.6?nM, 12.2?nM and 8.7?nM, respectively. Treatment with IACS-010759 robustly inhibited proliferation and induced apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS, likely owing to a combination of energy depletion and reduced aspartate production that leads to impaired nucleotide biosynthesis. KEYWORDS: IACS-010759 | supplier | OxPhos inhibitor | IACS-10759 | IACS 010759 | IACS010759 | IACS 10759 | IACS10759 | CAS [1570496-34-2] | NADH | NADH dehydrogenase | Inhibitor | Enzymes | OxPhos | Complex I | Brain cancer | AML

產(chǎn)品價格

現(xiàn)貨詢價，電話：010-67529703

產(chǎn)品規(guī)格

產(chǎn)品品牌

axonmedchem

產(chǎn)品概述

產(chǎn)品詳情

IACS-010759 - IACS-10759

Based on 4 reference(s) in Google Scholar 8 10 4

Axon 2909

CAS [1570496-34-2]

MF C25H25F3N6O4S
MW 562.56

Purity: 99%
Soluble in DMSO

IACS-010759

Description

IACS-010759 is an orally bioavailable, potent inhibitor of complex I of oxidative phosphorylation (OXPHOS). IACS-010759 was active in mouse, rat and cynomolgus monkey with IC50 values of 5.6?nM, 12.2?nM and 8.7?nM, respectively. Treatment with IACS-010759 robustly inhibited proliferation and induced apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS, likely owing to a combination of energy depletion and reduced aspartate production that leads to impaired nucleotide biosynthesis.

M Protopopova et al. Abstract 4380: IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities. Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015.

JR Molina et al. An inhibitor of oxidative phosphorylation exploits cancer vulnerability. Nat Med. 2018 Jul;24(7):1036-1046.

HV Vangapandu et al. Biological and metabolic effects of IACS-010759, an OxPhos inhibitor, on chronic lymphocytic leukemia cells. Oncotarget. 2018 May 18;9(38):24980-24991.

Certificate of Analysis
Material Safety Data Sheet

Apoptosis Cell Signaling & Oncology NADH dehydrogenase EC 1.6.5.11

Potent and orally bioavailable inhibitor of complex I of oxidative phosphorylation

Chemical name

5-(5-Methyl-1-(3-(4-(methylsulfonyl)piperidin-1-yl)benzyl)-1H-1,2,4-triazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole

Parent CAS No.

[1570496-34-2]

產(chǎn)品資料

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