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IACS-010759

产品编号 T5337 CAS 1570496-34-2

别名: IACS-10759, IACS 10759, IACS10759

IACS-010759 是一种口服有效的线粒体氧化磷酸化复合物 I 抑制剂。它在依赖 OXPHOS 的脑癌和急性髓性白血病模型中抑制增殖并诱导细胞凋亡，有研究复发/难治性 AML 和实体瘤潜力。

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IACS-010759, CAS 1570496-34-2

规格	价格/CNY	货期
1 mg	￥ 457	现货
2 mg	￥ 662	现货
5 mg	￥ 995	现货
10 mg	￥ 1,660	现货
25 mg	￥ 3,320	现货
50 mg	￥ 5,390	现货
100 mg	￥ 7,490	现货
200 mg	￥ 9,870	现货
500 mg	￥ 14,800	现货
1 mL * 10 mM (in DMSO)	￥ 1,230	现货

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其他形式的 IACS-010759:

Sobetirome
现货
IACS-010759 hydrochloride
询价

选择批次

纯度: 99.83%

纯度: 99.73%

纯度: 98.18%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	IACS-010759 is an orally bioavailable inhibitor of complex I of oxidative phosphorylation of the mitochondrial electron transport chain.
体外活性	Treatment of primary CLL cells with IACS-010759 greatly inhibited oxidative phosphorylation (OxPhos) but caused only minor cell death at 24 and 48 h [1]. KPS-tumor-derived murine cells were more sensitive to IACS-010759 compared to KP-tumor-derived cell lines [2]. Established AML cell lines were exposed to a range of IACS-010759 concentrations for 3–7 d, resulting in reduced viability with EC50 values of<3nM [3].
体内活性	In mice following intravenous (0.3mg per kg body weight (mg/kg)) and oral (1mg/kg) administration, IACS-010759 was characterized by low plasma clearance with a high volume of distribution, resulting in a prolonged terminal half-life (>24h) of IACS-010759 with sustained levels of compound in the plasma following oral dosing. Treatment with IACS-010759 at the 5 or 10mg/kg dose resulted in tumor regression with minimal body weight loss, whereas IACS-010759 at the 25mg/kg dose was not tolerated, and body weight loss, lethargy, and hypothermia were observed [3].
细胞实验	CLL cells were incubated with either dimethyl sulfoxide (control) or IACS-010759 (100 nM) for 24 h. A total of 10^6 cells were stained with MitoSOX Red and tetramethylrhodamine ethyl ester perchlorate and were analyzed using flow cytometry for mitochondrial reactive oxygen species (ROS) and mitochondrial outer membrane potential, respectively [1].
动物实验	OCI-AML3 cells were expanded in RPMI medium + 5% or 10% fetal bovine serum (FBS) until ≥150 million cells were present. For OCI-AML3, 2 million cells in 200 μl of saline were injection into the tail vein of NSG mice. For the patient-derived models, 4030094 and S6-AP, cells were harvested from mice with advanced disease or resuscitated from frozen vials, washed and resuspended at 5 x 10^6 cells/ml in PBS. Mice were irradiated for 24 hours at 250 cGY before orthotopic implantation of 1 x 10^6 cells suspended in 200 μl of saline were into the tail vein of 6- to 8-week old female NSG mice. For OCI-AML3, treatment began when whole body luminescence averaged 5 x 10^7. For model 4030094, treatment for the efficacy began when animals reached 10% burden and for the PK/PD studies when the animals reached 80% disease burden as measured by human and mouse CD45 and viability (DAPI 62248) staining followed by flow cytometry with a Fortessa flow cytometer. Mice were randomized based on luminescence for the OCI-AML3 model and by disease burden (hCD45+) for the patient-derived xenograft. Cohorts of mice were sacrificed 21 days after study drug initiation to collect spleen and bone marrow or followed for overall survival while continuing study drug [3].

别名	IACS-10759, IACS 10759, IACS10759
分子量	562.56
分子式	C25H25F3N6O4S
CAS No.	1570496-34-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 30 mg/mL (53.3 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7776 mL	8.8879 mL	17.7759 mL	44.4397 mL
	5 mM	0.3555 mL	1.7776 mL	3.5552 mL	8.8879 mL
	10 mM	0.1778 mL	0.8888 mL	1.7776 mL	4.444 mL
	20 mM	0.0889 mL	0.4444 mL	0.8888 mL	2.222 mL
	50 mM	0.0356 mL	0.1778 mL	0.3555 mL	0.8888 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Vangapandu HV, et al. Biological and metabolic effects of IACS-2010759, an OxPhos inhibitor, on chronic lymphocytic leukemia cells. Oncotarget. 2018 May 18;9(38):24980-241991. 2. Lissanu Deribe Y, et al. Mutations in the SWI/SNF complex induce a targetable dependence on oxidative phosphorylation in lung cancer. Nat Med. 2018 Jul;24(7):1047-1057. 3. Molina JR, et al. An inhibitor of oxidative phosphorylation exploits cancer vulnerability. Nat Med. 2018 Jul;24(7):1036-1046.

文献引用

1. Ren L, Meng L, Gao J, et al.PHB2 promotes colorectal cancer cell proliferation and tumorigenesis through NDUFS1-mediated oxidative phosphorylation.Cell Death & Disease.2023, 14(1): 44. 2. Hong J H, Yong C H, Heng H L, et al.Integrative multiomics enhancer activity profiling identifies therapeutic vulnerabilities in cholangiocarcinoma of different etiologies.Gut.2023 3. Hong J H, Yong C H, Heng H L, et al.Integrative multiomics enhancer activity profiling identifies therapeutic vulnerabilities in cholangiocarcinoma of different etiologies.Gut.2023

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

IACS-010759 1570496-34-2 Apoptosis Metabolism Others Mitochondrial Metabolism OXPHOS phosphorylation complex mitochondrial IACS-10759 Inhibitor orally IACS 010759 inhibit H460 AML IACS010759 IACS 10759 IACS10759 oxidative inhibitor

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IACS-010759

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords