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| 5mg |
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| 10mg |
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| Targets |
LDCA targets lactate dehydrogenase A (LDH-A), a key enzyme in the glycolytic pathway that catalyzes the conversion of pyruvate to lactate. By competitively inhibiting LDH-A enzyme activity, LDCA disrupts the metabolic reprogramming of cancer cells, which often rely on aerobic glycolysis (the Warburg effect). This inhibition alters mitochondrial hyperpolarization and triggers apoptosis in the malignant population. The compound shows significant effects in cancer cells without exhibiting toxicity.
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| ln Vitro |
When paired with doxorubicin, LDCA (2-100 μM; 16-72 h) works in concert to improve growth inhibition and trigger mitochondria by enlisting the caspase cascade, limiting migration, and removing the melanoma cells' capacity for clonal growth. apoptosis was mediated [1].
In vitro, LDCA is a dual-hit metabolic modulator that inhibits LDH-A enzyme activity to stimulate apoptosis in the malignant population. It shows significant anti-proliferative activity. The compound alters mitochondrial hyperpolarization and triggers apoptosis in cancer cells. These in vitro activities confirm its mechanism as a metabolic modulator that targets cancer cell metabolism. |
| ln Vivo |
In mouse melanoma models, LDCA (2 mg/kg, intravenously, once on day 6) in combination with doxorubicin reduces carcinogenic progression, stops tumor growth kinetics, and enhances survival [1].
Specific in vivo data for LDCA are limited in publicly available sources. Based on its in vitro mechanism, the compound is expected to have potential antitumor activity in vivo by targeting cancer cell metabolism. However, detailed in vivo efficacy studies in animal models have not been extensively reported. The compound is primarily used as a research tool. |
| Enzyme Assay |
In vitro enzyme assays for LDCA measure its inhibition of LDH-A enzyme activity. LDH-A is incubated with varying concentrations of the compound and its substrates (pyruvate and NADH). Enzyme activity is measured by monitoring the decrease in NADH absorbance at 340 nm. Competitive inhibition is determined from kinetic studies.
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| Cell Assay |
Cell viability assay [1]
Cell Types: B16-F10 Cell Tested Concentrations: 2-100 μM Incubation Duration: 72 h Experimental Results: Inhibits cell growth, has dose-dependent cytotoxicity, and has a strong synergistic effect with LDCA. Apoptosis analysis[1] Cell Types: B16-F10 Cell Tested Concentrations: 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: When cells were exposed to LDCA, it resulted in 15% death and synergistically with doxorubicin, resulting in 40% melanoma Cell death. Immunofluorescence[1] Cell Types: B16-F10 Cell Tested Concentrations: 20 μM Incubation Duration: 16 hrs (hours) Experimental Results: Demonstration that combination with doxorubicin affects cell morphology, leading to condensation and fragmentation of nuclei. Cell migration assay [1] Cell Types: B16-F10 Cell Tested Concentrations: 20 μM Incubation Duration: 16 hrs (hours) Experimental Results: Dramatically limited the migration potential of B16-F10 cells. Cell-based assays for LDCA are conducted in cancer cell lines. Cells are treated with the compound at various concentrations, and cell viability is assessed using MTT or similar assays. Mitochondrial membrane potential is measured using fluorescent dyes such as JC-1. Apoptosis is assessed by measuring caspase activation and other markers. These assays confirm the compound's anti-proliferative and pro-apoptotic effects. |
| Animal Protocol |
Animal/Disease Models: Melanoma tumor model [1]
Doses: 2 mg/kg Route of Administration: 2 mg/kg, intravenous (iv) (iv)injection, once on the 6th day. Experimental Results: Combined with doxorubicin, the survival ability of mice was Dramatically improved. , reduce tumor necrosis in mice. In vivo animal experiments with LDCA have not been extensively documented. Typical study designs would involve administration of the compound in xenograft models to evaluate antitumor efficacy. Dosing regimens and routes of administration would need to be optimized. The compound is for research use only. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of LDCA are not extensively characterized. The compound has a molecular formula of C8H5Cl3FNO and a molecular weight of 256.49. Appearance: Solid powder. Solubility: DMSO: 100 mg/mL (389.86 mM; Need ultrasonic). Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year.
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| Toxicity/Toxicokinetics |
Safety and toxicology data for LDCA indicate that it shows significant effects in cancer cells without exhibiting toxicity. The compound is for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
See also: Acetamide (note moved to).
LDCA has CAS number 349106-80-5, molecular formula C8H5Cl3FNO, and molecular weight 256.49. IUPAC name: 2,2-dichloro-N-(3-chloro-4-fluorophenyl)acetamide. It is a dual-hit metabolic modulator that inhibits LDH-A enzyme activity and stimulates apoptosis. Purity: 99.18%. Not for human use; for research purposes only. |
| Molecular Formula |
C8H5CL3FNO
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|---|---|
| Molecular Weight |
256.49
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| Exact Mass |
254.942
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| CAS # |
349106-80-5
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| PubChem CID |
4322881
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
215
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(NC1=CC=C(F)C(Cl)=C1)(=O)C(Cl)Cl
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| InChi Key |
WZVDWCGCAQYINC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H5Cl3FNO/c9-5-3-4(1-2-6(5)12)13-8(14)7(10)11/h1-3,7H,(H,13,14)
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| Chemical Name |
2,2-dichloro-N-(3-chloro-4-fluorophenyl)acetamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~389.88 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8988 mL | 19.4939 mL | 38.9879 mL | |
| 5 mM | 0.7798 mL | 3.8988 mL | 7.7976 mL | |
| 10 mM | 0.3899 mL | 1.9494 mL | 3.8988 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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