DCA (Sodium dichloroacetate)

别名: Dichloroacetic acid, bichloroacetic acid, BCA 中文名称:二氯乙酸钠

DCA (Sodium dichloroacetate)是 pyruvate dehydrogenase kinase (PDK) 的特异性抑制剂,对PDK2和PDK4的IC50值分别为183和80 μM;可抑制 Na+-K+-2Cl- cotransporter 和线粒体钾离子通道轴。Sodium dichloroacetate 可增加活性氧的生成,引起癌细胞凋亡,并抑制肿瘤生长。

DCA (Sodium dichloroacetate) Chemical Structure

DCA (Sodium dichloroacetate) Chemical Structure

CAS: 2156-56-1

规格 价格 库存 购买数量
100mg 794.47 现货
1g 3030.55 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

免费分装
免费预溶

DCA (Sodium dichloroacetate)相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
MCF7 Function assay 10 mM 12 hrs Inhibition of PDK1 in human MCF7 cells assessed as increase in oxygen consumption rate at 10 mM after 12 hrs 27006991
MCF7 Function assay 10 mM 12 hrs Inhibition of PDK1 in human MCF7 cells assessed as decrease in extracellular acidification rate at 10 mM after 12 hrs 27006991
MCF7 Function assay 10 mM 12 hrs Inhibition of PDK1 in human MCF7 cells assessed as decrease in proton production rate at 10 mM after 12 hrs 27006991
MCF7 Function assay 10 mM 12 hrs Inhibition of PDK1 in human MCF7 cells assessed as increase in ratio of oxygen consumption rate to extracellular acidification rate at 10 mM after 12 hrs 27006991
MCF7 Function assay 10 mM 12 hrs Inhibition of PDK1 in human MCF7 cells assessed as decrease in lactate production at 10 mM after 12 hrs 27006991
NCI-H1975 Antiproliferative assay 20 mM 72 hrs Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability at 20 mM after 72 hrs by MTT assay 30470491
MCF7 Antitumor assay 30 mg/kg two weeks Antitumor activity against human MCF7 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 30 mg/kg, iv administered every two days for two weeks measured after 14 days 31509699
MCF7 Function assay 30 uM 4 hrs Induction of metabolic reversal from aerobic glycolysis to oxidative phosphorylation in human MCF7 cells assessed as increase in extracellular acidification rate at 30 uM pretreated for 4 hrs followed by glucose addition after 25 mins by seahorse XF24 ext 31509699
MCF7 Function assay 30 uM 4 hrs Induction of metabolic reversal from aerobic glycolysis to oxidative phosphorylation in human MCF7 cells assessed as increase in extracellular acidification rate at 30 uM pretreated for 4 hrs followed by glucose addition after 25 mins followed by subsequent assay 31509699
MCF7 Function assay 30 uM 4 hrs Induction of metabolic reversal from aerobic glycolysis to oxidative phosphorylation in human MCF7 cells assessed as decline in extracellular acidification rate at 30 uM pretreated for 4 hrs followed by glucose addition after 25 mins followed by subsequent assay 31509699
MCF7 Function assay 30 uM 6 hrs Induction of metabolic reversal from aerobic glycolysis to oxidative phosphorylation in human MCF7 cells assessed as decrease in oxygen consumption rate at 30 uM pretreated for 6 hrs followed by oligomycin A addition after 25 mins followed by subsequent assay 31509699
MCF7 Function assay 90 mins Inhibition of PDK1 (unknown origin) expressed in human MCF7 cells using PDK tide as substrate measured after 90 mins in presence of ATP by ADP-Glo luminescent kinase assay 31509699
点击查看更多细胞系数据

生物活性

产品描述 DCA (Sodium dichloroacetate)是 pyruvate dehydrogenase kinase (PDK) 的特异性抑制剂,对PDK2和PDK4的IC50值分别为183和80 μM;可抑制 Na+-K+-2Cl- cotransporter 和线粒体钾离子通道轴。Sodium dichloroacetate 可增加活性氧的生成,引起癌细胞凋亡,并抑制肿瘤生长。
靶点
PDK4 [4]
(Cell-free assay)
PDK2 [4]
(Cell-free assay)
80 μM 183 μM
体外研究(In Vitro)
体外研究活性 DCA可引起人类肺部、乳腺和脑癌细胞的凋亡[1]。经DCA处理后,癌细胞中的ROS水平升高、MMP去极化、在体内外都能够增加凋亡[2]。DCA抑制丙酮酸脱氢酶激酶(PDK)的活性,因而刺激线粒体丙酮酸脱氢酶(PDH)。当PDH处于关闭状态时,PDH不再将丙酮酸转化为acetyl-CoA(线粒体呼吸和葡萄糖依赖的氧化磷酸化过程所必需)。从而,DCA将细胞代谢从糖酵解转换为葡萄糖氧化,降低线粒体膜电位,促进线粒体转运孔的开放。这一系列代谢转换有助于促凋亡介质如cyt c和AIF的易位。因而,DCA可通过凋亡反应驱动癌细胞自杀[3]
细胞实验 细胞系 乳腺癌细胞
浓度 5 mM
孵育时间 24-72 h
方法

将细胞以3000细胞/孔的密度铺于96孔板。用DCA和ATO处理24-72小时,然后换成新鲜的含30 μg/ml的中性红培养基孵育3小时。PBS洗涤细胞,加入lysis buffer(acetic acid/methanol, 80%/20%),在540 nm处检测吸光值。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot pPDH E1α / PDH E1α 25630799
体内研究(In Vivo)
体内研究活性 DCA在体内体外可作为细胞生长抑制剂,而不引起程序性细胞死亡(凋亡)。DCA是一种安全性较高的药物,没有心脏、肺部、肾脏或骨髓毒性。最为严重的副作用包括周围神经病变,该作用为可逆过程。DCA在好几种癌症类型中,包括结肠癌、前列腺癌、卵巢癌、成神经细胞瘤、肺癌、子宫颈癌、子宫内膜、胆管癌、肉瘤和T细胞淋巴瘤具有抗癌活性。DCA的其他一些抗肿瘤作用也被报导,包括阻碍血管生成、改变HIF-1α的表达、pH调节剂V-ATPase和MCT1的改变、其他细胞生存调节子如PUMA、GLUT1、Bcl2和p53的改变。在大鼠高转移乳腺癌模型中,DCA能够显著地减少肺部转移性负担[1]。在C57BL/6小鼠中,DCA-Na的体内给药可诱导20%的生存率提高并减少肿瘤直径、体积和重量,而不影响其体重、并避免转移[3]
动物实验 Animal Models C57BL/6 mice
Dosages 500 and 1000 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06073106 Not yet recruiting
Stroke|Traumatic Brain Injury|Knee Osteoarthritis|Breast Cancer
Tan Tock Seng Hospital|Rehabilitation Research Institute of Singapore (RRIS)|Woodlands Health (WH)
December 2023 --
NCT05810623 Not yet recruiting
Upper Urinary Tract Urothelial Carcinoma|Bladder Cancer
David D''Andrea|Medical University of Vienna
June 1 2023 Phase 3
NCT05646485 Recruiting
Bladder Cancer|Urothelial Carcinoma|Hematuria|Smoking Cessation
University of Texas Southwestern Medical Center
May 5 2023 Not Applicable
NCT05460533 Recruiting
B-cell Acute Lymphoblastic Leukemia
Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals
July 12 2022 Phase 2

化学信息&溶解度

分子量 150.92 分子式

C2HCl2O2.Na

CAS号 2156-56-1 SDF Download DCA (Sodium dichloroacetate) SDF
Smiles C(C(=O)[O-])(Cl)Cl.[Na+]
储存条件(自收到货起)

体外溶解度
批次:

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

* 必填项

请输入您的姓名
请输入您的邮箱地址 请输入一个有效的邮箱地址
请写点东西给我们
Tags: buy DCA (Sodium dichloroacetate) | DCA (Sodium dichloroacetate) supplier | purchase DCA (Sodium dichloroacetate) | DCA (Sodium dichloroacetate) cost | DCA (Sodium dichloroacetate) manufacturer | order DCA (Sodium dichloroacetate) | DCA (Sodium dichloroacetate) distributor
在线咨询
联系我们