IACS-010759 (IACS-10759)

For research use only. Not for use in humans.

目录号：S8731

IACS-010759 (IACS-10759) Chemical Structure

CAS No. 1570496-34-2

IACS-010759 (IACS-10759)是一种有效的、选择性氧化磷酸化 (oxidative phosphorylation) 抑制剂，IC50小于10 nM，它通过抑制complex I阻止细胞呼吸作用。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2366.91 现货
RMB 1286.57 现货
RMB 4153.2 现货
RMB 9583.25 现货
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客户使用Selleck生产的IACS-010759 (IACS-10759)发表文献9篇：

产品安全说明书

OXPHOS抑制剂选择性比较

生物活性

产品描述 IACS-010759 (IACS-10759)是一种有效的、选择性氧化磷酸化 (oxidative phosphorylation) 抑制剂，IC50小于10 nM，它通过抑制complex I阻止细胞呼吸作用。
靶点
oxidative phosphorylation [2]
()
10 nM
体外研究

在检测细胞中（Notch突变株:Pf382, 1301, Jurkat, MOLT-4, P12-Ichikawa和Notch野生型T-ALL1），IACS-010759显著地降低了细胞活力。对T-ALL处理以IACS-010759能有效地抑制脂肪酸刺激的线粒体呼吸，而细胞仍可以通过糖酵解产生能量[1]。在CLL细胞中，IACS-010759引起较少的细胞死亡，抑制耗氧率并增加糖酵解。IACS-010759降低了细胞内核糖核苷三磷酸[2]。在敏感性AML细胞中，IACS-010759诱导AMPK的激活、抑制mTOR，导致细胞生长受到抑制。AMPK和mTOR可作为IACS-010759抗白血病活性的生物标记[3]。
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Z-138 MlfNVJJwdGmoZYLheIlwdiCjc4PhfS=> NFT3ZZU4OiCq MXvJRWNUNTBzMEe1PUBqdmirYnn0[YQhfGinIIDyc4xq\mW{YYTpc44hd2ZiWj2xN|ghcW5iYTDkc5Nm\GWyZX7k[Y51KG2jbn7ldkBifCCwYX7vcY9t[XJiY3;uZ4VvfHKjdHnvcpM> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTB4OES0NEc,OzFyNki0OFA9N2F-
Maver-1 NUTjWIZWWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4fZVVczKGh? NEPWXVhKSUOVLUCxNFc2QSCrbnjpZol1\WRidHjlJJBzd2yrZnXyZZRqd25ib3[gUYF3\XJvMTDpckBiKGSxc3Xk[ZBmdmSnboSgcYFvdmW{IHH0JI5idm:vb3zhdkBkd26lZX70doF1cW:wcx?= M3L3elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzME[4OFQxLz5|MUC2PFQ1ODxxYU6=
H1975 M2K1THBzd2yrZnXyZZRqd25iYYPzZZk> MnHqNkBl[Xm| MmrqbIF{KGyrbXn0[YQh\W[oZXP0JI9vKGOnbHygdJJwdGmoZYLheIlwdg>? MkDRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB4MkWzNlkoRjNyNkK1N|I6RC:jPh?=
CLL cells Mkn2SpVv[3Srb36gZZN{[Xl? MYSxNFAhdk1? NVPCXGw5OjRiaB?= M2PxdYlvcGmkaYTzJG9EWiCjbnSgbY5kemWjc3XzJIdtgWOxbInzbZMhcW5iQ1zMJINmdGy| NUXubmlrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4OlE5PDdpPkK5PFYyQDR5PD;hQi=>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
Cyto c / VDAC1 / β-Actin; 

PubMed: 32847115     


IACS-010759 and venetoclax cooperatively induce intrinsic apoptosis. (a) MV4-11 cells cultured in media supplemented with glucose were treated with vehicle control, IACS-010759, venetoclax, or in combination for 4 or 8 h. Cellular fractionation was performed. Mitochondrial and cytosolic fractions were subjected to western blot analysis. This experiment was performed 2 independent times in triplicate. One representative image is shown.

Cleaved PARP / Cleaved Caspase 3 / GAPDH; 

PubMed: 29861847     


(F) Immunoblot showing cleaved PARP and cleaved caspase 3 proteins in untreated or treated cells. C; Control untreated; D, drug IACS-010759-treated. Glyceraldehyde 3-phosphate dehydrogenase (GAPDH) protein was used as loading control.

Actin / LC3B I / LC3B II; 

PubMed: 32792483     


(h) Viable bone marrow AML blasts from mice treated with IACS-010759 (one experiment) were subjected to Western blot analysis for actin and LC3B. Numbers indicate ratios obtained by densitometric analysis.

32847115 29861847 32792483
Growth inhibition assay
Tumor Volume; 

PubMed: 32581056     


8 Gy×3 might be the most optimal radiotherapy (XRT) dose and fractionation scheme when combined with IACS-010759. Mice (six per group) were injected subcutaneously with 1×105 PD-1-resistant cells into the right leg and tumors were harvested on day 18. Three radiation schemes were chosen for comparison: 12 Gy×2 fractions, 8 Gy×3 fractions, and 6 Gy×3 fractions. IACS-010759 was administrated as per the protocol described in the text. Thus, the experiment had eight groups: control, IACS-010759 alone, 12 Gy×2 XRT, 8 Gy×3 XRT, 6 Gy×3 XRT, 12 Gy×2 XRT combined with IACS-010759, 8 Gy×3 XRT combined with IACS-010759, and 6 Gy×3 XRT combined with IACS-010759. (A) Data are presented according to XRT scheme. Only 8 Gy×3 combined with IACS-010759 showed significantly increased efficacy compared with XRT alone (two-way ANOVA, p=0.003).

32581056
IHC
pimonidazole stain; 

PubMed: 30787016     


(B) Representative pimonidazole staining analysis results of ICr A375-R1 xenografts treated for 1 week with IACS-010759 (5 mg/kg PO once daily) or vehicle.

pimonidazole stain of skull section; 

PubMed: 32695673     


Evaluation of the effect of Complex I inhibitor (OxPhosi) on BM hypoxia using pimonidazole IHC. (A,C) representative IHC of skull section of untreated leukemic mouse and (B,D) IHC of skull section of IACS-010759 treated mouse.

H&E stain; 

PubMed: 32695673     


Evaluation of the effect of Complex I inhibitor (OxPhosi) on BM hypoxia using pimonidazole IHC. (E,F) H&E on corresponding adjacent sections.

30787016 32695673
Immunofluorescence
Bodipy 493-503 / DAPI; 

PubMed: 32792483     


(e) Viable bone marrow AML blasts from mice treated with IACS-010759 were stained for Bodipy 493/503 and DAPI. Scale bar: 10 µm.

VDAC1 : IP3R1; 

PubMed: 32792483     


(i) Purified viable bone marrow AML blasts from mice treated with IACS-010759 (one experiment) were subjected to PLA assay.

32792483

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验：

[2]
- 合并
  • Cell lines: CLL细胞
  • Concentrations: 30 nM, 100 nM, 300 nM, 1 μM, 3 μM
  • Incubation Time: 24 或 48 h
  • Method:

    用IACS-010759处理CLL细胞24或48小时，收集细胞，吖啶橙染色后，进行流式分析。


    (Only for Reference)

溶解度 (25°C)

体外 DMSO 27 mg/mL (47.99 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 562.56
化学式

C25H25F3N6O4S
CAS号 1570496-34-2
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID