| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Galloflavin targets lactate dehydrogenase (LDH), a key enzyme in the glycolytic pathway that catalyzes the conversion of pyruvate to lactate, regenerating NAD+ in the process. LDH-A is upregulated in many cancers and is associated with the Warburg effect, where cancer cells rely on aerobic glycolysis for energy production. By inhibiting LDH, galloflavin disrupts glycolysis and reduces lactate production, leading to metabolic stress and apoptosis in cancer cells. Its selectivity for LDH over other dehydrogenases supports its use as a specific probe for studying cancer metabolism.
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| ln Vitro |
Pentaflavin participates in several signaling pathways that control metabolism, cell cycle, apoptosis, cell stress, and metastasis, hence successfully inhibiting cell growth in endometrial cancer cell lines and human endometrial cancer primary cultures [3].
In vitro, galloflavin demonstrates potent inhibition of LDH-A and LDH-B with IC50 values of 5.46 µM and 10.4 µM, respectively. In cell-based assays, galloflavin inhibits the proliferation of cancer cell lines and induces apoptosis. The compound's activity is concentration-dependent, with effective concentrations typically in the micromolar range. Its inhibition of LDH disrupts glycolysis, reducing ATP production and increasing oxidative stress in cancer cells. Galloflavin's ability to target cancer metabolism makes it a valuable tool for studying the Warburg effect and for developing novel anticancer therapeutics. |
| ln Vivo |
In vivo, galloflavin has been studied in preclinical models of cancer. Its ability to inhibit LDH and disrupt cancer metabolism may lead to antitumor effects. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying cancer metabolism. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro LDH inhibition assay for galloflavin typically uses purified LDH enzyme and measures the conversion of pyruvate to lactate. The assay is performed in 96-well plates with NADH, pyruvate, and varying concentrations of the test compound (typically 0.1 to 100 µM). The reaction is initiated by adding the enzyme, and the decrease in absorbance at 340 nm is monitored over time. IC50 values are calculated from dose-response curves using nonlinear regression. Positive controls (e.g., known LDH inhibitors) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, cancer cell lines (e.g., HeLa, MCF-7) are treated with galloflavin at concentrations ranging from 0.1 to 100 µM for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Lactate production is measured using a colorimetric or fluorometric assay. ATP levels are measured using a luciferase-based assay. Apoptosis is quantified by Annexin V/PI staining and caspase activity assays. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo efficacy studies, immunodeficient mice are subcutaneously inoculated with cancer cells. When tumors reach a volume of approximately 100-200 mm³, mice are randomized into treatment groups (n=5-10 per group). Galloflavin is administered intraperitoneally or orally at doses ranging from 1 to 50 mg/kg, typically once or twice daily, for 14-28 days. Tumor volume is measured twice weekly using calipers, and body weight is monitored for toxicity. At study endpoint, tumors are harvested for metabolic analysis and immunohistochemistry. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of galloflavin have been partially characterized. Following intraperitoneal administration, the compound shows moderate absorption with a Tmax of 0.5-2 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including tumor, liver, and kidney. Metabolism is primarily hepatic, with oxidation and conjugation as major pathways. The compound is eliminated primarily via biliary and renal excretion. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of galloflavin are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References |
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| Additional Infomation |
Galloflavin is a potent LDH inhibitor with IC50 values of 5.46 µM (LDH-A) and 10.4 µM (LDH-B). It inhibits cancer cell metabolism and induces apoptosis. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥95%) for laboratory use only. Its LDH inhibition makes it a valuable tool for studying cancer metabolism and for developing novel anticancer therapeutics.
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| Molecular Formula |
C12H6O8
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|---|---|
| Molecular Weight |
278.1712
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| Exact Mass |
278.006
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| CAS # |
568-80-9
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| Related CAS # |
Galloflavin potassium; 1780260-20-9
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| PubChem CID |
135483971
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| Appearance |
Brown to breen solid powder
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| Density |
2.1g/cm3
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| Boiling Point |
159.8ºC at 760 mmHg
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| Flash Point |
37.4ºC
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| Index of Refraction |
1.848
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| LogP |
0.721
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
20
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| Complexity |
729
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(C2=C([H])C(C(=C(C2=C2C1=C([H])C(=C(O[H])O2)O[H])O[H])O[H])=O)=O
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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 : ~10 mg/mL (~35.95 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (5.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 0.5 mg/mL (1.80 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 DMSO stock solution (5.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: 0.5 mg/mL (1.80 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Suspended solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (5.0 mg/mL) to 900 μL of corn oil and mix well. View More
Solubility in Formulation 4: 25 mg/mL (89.87 mM) in 50% PEG300 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), Suspended solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5949 mL | 17.9746 mL | 35.9492 mL | |
| 5 mM | 0.7190 mL | 3.5949 mL | 7.1898 mL | |
| 10 mM | 0.3595 mL | 1.7975 mL | 3.5949 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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