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Dichloroacetate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dichloroacetate图片
CAS NO:2156-56-1
规格:≥98%
包装与价格:
包装价格(元)
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 150.92
Formula C2HCl2O2.Na
CAS No. 2156-56-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 30 mg/mL (198.78 mM)
Water: 30 mg/mL (198.78 mM)
Ethanol: 30 mg/mL (198.78 mM)
SMILES O=C([O-])C(Cl)Cl.[Na+]
Synonyms Bichloroacetic acid, BCA; Sodium Dichloroacetate; CPC-211; DCA; X-11S
实验参考方法
In Vitro

In vitro activity: DCA can trigger apoptosis of human lung, breast and brain cancer cells. Cancer cells shows increased levels of ROS, depolarization of the MMP in vitro and increased apoptosis both in vitro and in vivo after DCA treatment. DCA inhibits the activity of pyruvate dehydrogenase kinase (PDK), thereby stimulating the mitochondrial enzyme pyruvate dehydrogenase (PDH). When turned off, PDH no longer converts pyruvate to acetyl-CoA required for mitochondrial respiration and glucose dependent oxidative phosphorylation. DCA shifts cellular metabolism from glycolysis to glucose oxidation, decreasing the mitochondrial membrane potential gradient and helping to open mitochondrial transition pores. This metabolic switch facilitates translocation of pro-apoptotic mediators like cytochrome c (cyt c) and apoptosis inducing factor (AIF), both of which stimulate apoptosis. DCA thus drives cancer cells to commit suicide by apoptosis.


Kinase Assay: Dichloroacetate (CPC-211; DCA; X-11S) is a potent and specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively.


Cell Assay: In order to assess cell viability, cells are plated in 96 well plates at a density of 3000 cells per well and 8 wells per group. Following exposure to DCA and ATO for 24 to 72 hours, cells are incubated for 3 hours with neutral red (30 μg/ml) in fresh media, then washed with PBS, followed by the addition of lysis buffer (acetic acid/methanol, 80%/20%) and the absorbance at 540 nm is recorded. Results are expressed as mean ± S.D, calculations are performed using the Prism software package, ANOVA with Tukey post test was applied and P < 0.05 was considered to be statistically significant.

In VivoDCA is discovered to be a safe drug with no cardiac, pulmonary, renal or bone marrow toxicity. The most serious common side effect is peripheral neuropathy, which is reversible. DCA has anti-cancer activity in several cancer types including colon, prostate, ovarian, neuroblastoma, lung carcinoid, cervical, endometrial, cholangiocarcinoma, sarcoma and T-cell lymphoma. Other antineoplastic actions of DCA have also been suggested. Which include angiogenesis blockade, changes in expression of HIF1-α, alteration of pH regulators V-ATPase and MCT1, and other cell survival regulators such as PUMA, GLUT1, Bcl2 and p53. DCA can significantly reduce metastatic burden in the lungs of rats in a highly metastatic in vivo model of breast cance.In vivo the DCA-Na treatment induces 20% survival and decreased the tumoral diameter, volume and weight, without affect the body weight and avoid metastasis in C57BL/6 mice.
Animal model C57BL/6 mice
Formulation & Dosage saline; 500 and 1000 mg/kg; i.p.
References World J Clin Cases. 2016 Oct 16;4(10):336-343; Mol Cancer. 2011 Nov 18;10:142; J Biol Chem. 2014 Feb 14;289(7):4432-43.