IACS-010759 | IACS-10759 | OXPHOS Inhibitor | AmBeed-信号通路专用抑制剂

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IACS-010759 {[allProObj[0].p_purity_real_show]}

货号：A857297 同义名： IACS-10759

IACS-010759 是一种口服有效的线粒体氧化磷酸化复合体 I (OXPHOS) 抑制剂。IACS-010759 抑制增殖并诱导 OXPHOS 依赖性脑癌和急性髓性白血病 (AML) 模型中的凋亡。IACS-010759 在复发/难治性 AML 和实体瘤研究中具有潜力。

IACS-010759 化学结构
CAS号：1570496-34-2

IACS-010759 3D分子结构
CAS号：1570496-34-2

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IACS-010759 纯度/质量文件产品仅供科研

货号：A857297 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

IACS-010759 生物活性

描述

OxPhos (oxidative phosphorylation) is an energy-efficient way of synthesizing ATP in the mitochondria which is a predominant pathway in CLL (chronic lymphocytic leukemia) for energy production and is further augmented in the presence of the stromal microenvironment. IACS-010759, currently in clinical development, is a small-molecule, orally bioavailable OxPhos inhibitor that targets mitochondrial complex I at low nanomolar levels. Treatment of primary CLL cells with 100 nM IACS-010759 greatly inhibited OxPhos but caused only minor cell death at 24 and 48 h. In 100 nM IACS-010759-treated CLL cells, basal OCR (oxygen consumption rate, a measure of OxPhos) was greatly inhibited followed by a drastic decrease in spare respiratory capacity (after addition of FCCP, a kind of uncoupler) compared with the untreated control. CLL cells were incubated with 100 nM IACS-010759 for 24 h (n = 19) and 48 h (n = 6). The ribonucleotide pools decreased at both time points upon drug treatment. ATP concentrations in CLL cells from these patients ranged from 693 to 5267 μM with a mean of 2775 μM. This mean value decreased to 1652 μM after 24 h. At 48 h, the levels further decreased from 2124 to 943 μM. In CLL cells incubated with the combination of 100 nM IACS-010759 and 2-dG, the OCR was further and significantly reduced compared with controls and even compared with cells treated with IACS-010759 alone^[1].

IACS-010759 参考文献

[1]Biological and metabolic effects of IACS-010759, an OxPhos inhibitor, on chronic lymphocytic leukemia cells

IACS-010759 实验方案

计算器

存储液制备

1mg

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1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.89mL

1.78mL

0.89mL

17.78mL

3.56mL

1.78mL

IACS-010759 技术信息

CAS号	1570496-34-2
分子式	C₂₅H₂₅F₃N₆O₄S
分子量	562.564

别名	IACS-10759
运输	蓝冰

存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(88.88 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

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浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

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全球学术期刊中引用的产品

IACS-010759 质控信息

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IACS-010759 参考文献

IACS-010759 实验方案

IACS-010759 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

细胞研究

临床研究

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