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Chemical Structure| 2156-56-1 Chemical Structure| 2156-56-1

Structure of Sodium dichloroacetate
CAS No.: 2156-56-1

Chemical Structure| 2156-56-1

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Sodium dichloroacetate is a metabolic regulator in cancer cell mitochondria with anticancer activity. It reduces lactate in the tumor microenvironment by inhibiting pyruvate dehydrogenase kinase (PDHK), increases reactive oxygen species (ROS) production, promotes cancer cell apoptosis, and can act as an NKCC inhibitor.

Synonyms: DCA; Dichloroacetic acid; X-11S

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Product Details of Sodium dichloroacetate

CAS No. :2156-56-1
Formula : C2HCl2NaO2
M.W : 150.92
SMILES Code : O=C([O-])C(Cl)Cl.[Na+]
Synonyms :
DCA; Dichloroacetic acid; X-11S
MDL No. :MFCD00070489
InChI Key :LUPNKHXLFSSUGS-UHFFFAOYSA-M
Pubchem ID :517326

Safety of Sodium dichloroacetate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
PC3 cells 80 µM 24 hours To observe the effect of DCA on PC3 cells, it was found that DCA induced autophagy, increased LC3B II expression, reduced lactate excretion, and decreased kPL. Br J Cancer. 2014 Jul 15;111(2):375-85.
HCT116 WT cells 75 µM 24 hours To observe the effect of DCA on HCT116 WT cells, it was found that DCA induced autophagy, increased LC3B II expression, reduced lactate excretion, and decreased kPL. Br J Cancer. 2014 Jul 15;111(2):375-85.
HT29 cells 100 µM 24 hours To observe the effect of DCA on HT29 cells, it was found that DCA induced autophagy, increased LC3B II expression, reduced lactate excretion, and decreased kPL. Br J Cancer. 2014 Jul 15;111(2):375-85.
Astroglia 100 µM 60 minutes Dichloroacetate significantly stimulated glucose and lactate oxidation in astroglia, increasing glucose oxidation by 34% (P<0.01) and lactate oxidation by 36% (P<0.01), and reduced lactate release by 20% (P<0.01). Proc Natl Acad Sci U S A. 2003 Apr 15;100(8):4879-84.
Neurons 100 µM 60 minutes Dichloroacetate had small effects on glucose and lactate oxidation in neurons, increasing glucose oxidation by 15% (P<0.05) and lactate oxidation by 11% (statistically insignificant). Proc Natl Acad Sci U S A. 2003 Apr 15;100(8):4879-84.
KYSE-410 cells 10, 20, 40 mM 72 hours Analyze the effect of dichloroacetate on hyaluronan (HA) synthesis in KYSE-410 cells, showing a dose-dependent increase in HA deposition Br J Pharmacol. 2019 Dec;176(23):4474-4490.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Tumor xenograft model Oral administration in drinking water 0.3 g/L Daily administration for 60 days Evaluate the antitumor effect of dichloroacetate in a nude Mice tumor xenograft model, showing significant inhibition of tumor growth Br J Pharmacol. 2019 Dec;176(23):4474-4490.
Mice Lewis lung carcinoma xenograft model Drinking water 1.5 g/L 8 days Significantly suppressed macrophage accumulation in tumor tissue Nat Commun. 2016 May 18;7:11635
NCr nude mice HT29 xenograft model Oral 200 mg/kg Once daily for 4 days To observe the effect of DCA on HT29 xenografts, it was found that DCA induced autophagy, increased LC3B II expression, and decreased kPL. Br J Cancer. 2014 Jul 15;111(2):375-85.
NSG mice HSJD-DIPG007 xenograft model Oral 250 mg/kg Twice daily until the end of the experiment To evaluate the therapeutic effect of the triple combination of DCA, metformin, and radiation therapy on the HSJD-DIPG007 xenograft model, results showed that the triple combination significantly prolonged the survival of mice. Neuro Oncol. 2020 Jan 11;22(1):139-151
Rats Sprague-Dawley rats Intravenous injection 50 mg/kg Single dose, over 5 minutes Dichloroacetate significantly lowered arterial plasma lactate levels (?29%, P<0.01) and glucose levels (?13% to ?18%, P<0.01), and increased baseline glucose utilization (lCMRglc) throughout the brain. Additionally, dichloroacetate reduced the percent increases in lCMRglc evoked by functional activation. Proc Natl Acad Sci U S A. 2003 Apr 15;100(8):4879-84.
Nude mice Intracranial GB and MB models Oral 100 mg/kg Twice daily for 32 days (GB model) or 34 days (MB model) Triplet therapy significantly inhibited intracranial tumor growth and extended survival in MB models. Mol Oncol. 2023 Sep;17(9):1803-1820.

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