| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Bcl-xL; Survivin; XIAP
Flavokawain A targets multiple cellular pathways involved in cancer progression and inflammation. It regulates Bax protein-dependent and mitochondrial-dependent apoptotic pathways, inducing apoptosis in cancer cells. It also modulates signaling pathways related to inflammation and oxidative stress. The compound has been shown to have protective activity against oxidative stress. |
|---|---|
| ln Vitro |
Flavokawain A induces apoptosis of bladder cancer cells and inhibits tumor growth in mice. It regulates Bax protein-dependent and mitochondrial-dependent apoptotic pathways. The compound's anticancer activity has been demonstrated in various cancer cell lines. It also exhibits anti-inflammatory effects by modulating signaling pathways related to inflammation.
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| ln Vivo |
Flavokawain A has been shown to inhibit tumor growth in mice. Its anticancer and anti-inflammatory properties have been studied in various animal models. The compound's ability to induce apoptosis and regulate mitochondrial pathways contributes to its in vivo efficacy. It has also been studied for its protective activity against oxidative stress induced by ochratoxin A.
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| Enzyme Assay |
For non-cellular assays, flavokawain A's antioxidant activity can be evaluated using DPPH radical scavenging and ABTS assays. Its binding to target proteins can be assessed using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). The compound's effect on mitochondrial function can be assessed using isolated mitochondria and measuring parameters such as membrane potential and cytochrome c release.
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| Cell Assay |
In vitro cellular assays for flavokawain A involve treating cancer cells (e.g., bladder cancer cells) with the compound and assessing cell viability, apoptosis, and signaling pathways. Cell viability is measured using MTT or CellTiter-Glo® assays. Apoptosis is assessed by flow cytometry using Annexin V/PI staining or by measuring caspase activity. The regulation of Bax and mitochondrial pathways is assessed by Western blotting.
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| Animal Protocol |
In vivo animal experiments with flavokawain A involve administering the compound to mouse xenograft models of cancer. Tumor-bearing mice are treated with flavokawain A via oral gavage or intraperitoneal injection, and tumor growth inhibition is monitored. Endpoints include tumor volume measurements, histopathological analysis, and assessment of apoptosis markers in tumor tissue. The compound's effects on oxidative stress are assessed in models of toxin-induced injury.
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| ADME/Pharmacokinetics |
Flavokawain A has a molecular weight of 314.33 and a molecular formula of C₁₈H₁₈O₅. It is a solid at room temperature and is typically stored at -20°C, protected from light. The compound is soluble in DMSO and other organic solvents. Purity is typically ≥98%. It is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Toxicological data for flavokawain A are limited. As a natural product, it is generally considered to have low toxicity, but high doses may cause adverse effects. Kava extracts, from which flavokawain A is derived, have been associated with hepatotoxicity, although the role of specific kavalactones and chalcones in this toxicity is not fully understood.
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| References | |
| Additional Infomation |
Flavokawain A belongs to the chalcone class of compounds. 2'-Hydroxy-4,4',6'-Trimethoxychalcone has been reported in turmeric (Boesenbergia rotunda), Vitex quinata, and other organisms with available data. See also: Roots (parts) of Piper methysticum.
Flavokawain A is a naturally occurring chalcone from the kava plant with anticancer and anti-inflammatory properties. It induces apoptosis in cancer cells and inhibits tumor growth in mice. It also exhibits protective activity against oxidative stress. The compound is available from various commercial suppliers for research applications. |
| Molecular Formula |
C18H18O5
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|---|---|
| Molecular Weight |
314.33252
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| Exact Mass |
314.115
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| CAS # |
64680-84-8
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| Related CAS # |
64680-84-8
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| PubChem CID |
5355469
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| Appearance |
Light yellow to yellow solid
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| Melting Point |
113 °C
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| LogP |
3.314
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
23
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| Complexity |
400
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=C(C=C1)C=CC(=O)C2=C(C=C(C=C2OC)OC)O
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| InChi Key |
CGIBCVBDFUTMPT-RMKNXTFCSA-N
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| InChi Code |
InChI=1S/C18H18O5/c1-21-13-7-4-12(5-8-13)6-9-15(19)18-16(20)10-14(22-2)11-17(18)23-3/h4-11,20H,1-3H3/b9-6+
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| Chemical Name |
(E)-1-(2-hydroxy-4,6-dimethoxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one
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| Synonyms |
Flavokawain A
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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: 25~43 mg/mL (79.5~136.8 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1814 mL | 15.9068 mL | 31.8137 mL | |
| 5 mM | 0.6363 mL | 3.1814 mL | 6.3627 mL | |
| 10 mM | 0.3181 mL | 1.5907 mL | 3.1814 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.