| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Multiple targets: flavone exhibits antioxidant, anti-inflammatory, antimicrobial, and anticancer activities. Anticancer mechanisms include direct antioxidant activity, quenching free radicals, bolstering endogenous defenses, modulation of PI3K/AKT/mTOR pathway, induction of mitochondrial apoptosis, and inhibition of Nrf2 signaling. Also modulates MAPK-dependent apoptosis.
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| ln Vitro |
Flavones have shown promise in anticancer drug advancement. Flavone and derivatives induce apoptosis in cancer cells via mitochondrial pathway, target PI3K/AKT/mTOR, inhibit Nrf2 signaling, modulate MAPK-dependent apoptosis. Increase cytotoxicity of NK cells in non-small cell lung cancer cells. Anticancer mechanisms range from direct antioxidant activity to pleiotropic pharmacological effects against cancer progression.
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| ln Vivo |
In vivo, flavone and derivatives show anti-tumor activity in colon cancer and non-small cell lung cancer models. Dietary flavonoids exhibit pleiotropic pharmacological strengths against cancer progression. Flavone derivatives inhibit growth of colon cancer xenografts in nude mice, reduce tumor volume, induce apoptosis. Flavone itself less studied in vivo than derivatives; further research may create more potent cancer treatments.
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| Enzyme Assay |
(1) DPPH assay: mix flavone with DPPH solution, incubate 30 min, measure OD517. (2) ABTS radical scavenging assay. (3) COX-2 inhibition: incubate recombinant COX-2 (0.1 U) with arachidonic acid (10 uM) and flavone (0.1-100 uM) in 50 mM Tris-HCl pH8.0, measure PGE2 by ELISA.
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| Cell Assay |
(1) Seed cancer cells (HT-29, A549, HeLa) at 5,000-10,000/well in 96-well plates. (2) Treat with flavone (0.1-100 uM) for 48-72 h. (3) Add MTT/CCK-8, calculate IC50. (4) For apoptosis: treat 48 h, stain Annexin V-FITC/PI, flow cytometry. (5) For cell cycle: treat 24-48 h, fix in 70% ethanol, stain with PI (50 ug/mL)+RNase A (100 ug/mL), FACS. (6) For mechanism: treat with flavone (10-50 uM) for 6-24 h, lyse, Western blot for Bcl-2, Bax, cleaved caspase-3, PARP, and PI3K/AKT/mTOR or MAPK markers.
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| Animal Protocol |
(1) For anti-tumor: use BALB/c nude mice (20-25 g) bearing HT-29 or A549 xenografts (100-150 mm3). (2) Administer flavone IP (50-200 mg/kg) or oral (100-500 mg/kg) daily or every other day for 14-28 days. (3) Formulation: for IP, dissolve in 10% DMSO/40% PEG300/5% Tween-80/45% saline; for PO, suspend in 0.5% CMC-Na+0.1% Tween-80. (4) Monitor tumor volume and body weight twice weekly. (5) At endpoint, excise tumors, weigh, histology (H&E, IHC for Ki-67, cleaved caspase-3, CD31), TUNEL, and Western blot for apoptosis markers. (6) Collect blood for serum chemistry and cytokines (TNF-alpha, IL-6).
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| ADME/Pharmacokinetics |
Soluble in DMSO (≥20 mg/mL, 90.7 mM) and ethanol; very low water solubility (<0.1 mg/mL). For cell culture, prepare 10-100 mM stock in DMSO, dilute into medium (final DMSO ≤0.1%). For IP, prepare 10-20 mg/mL in 10% DMSO/40% PEG300/5% Tween-80/45% saline. For PO, suspend in 0.5% CMC-Na+0.1% Tween-80. Storage: powder at -20degC for 3 years, protect from light.
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| Toxicity/Toxicokinetics |
In vitro: CCK-8 on HEK293 cells with flavone 1-200 uM, 48 h, IC50 >100 uM. In vivo: acute oral LD50 in mice >1000 mg/kg; IP LD50 ~500-1000 mg/kg. High doses (>200 mg/kg IP) cause mild sedation, weight loss, GI distress. No significant hepatotoxicity, nephrotoxicity, or carcinogenicity at therapeutic doses. For research only.
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| Additional Infomation |
Flavonoids are the simplest members of the flavonoid family, consisting of a 4H-chromen-4-one with a phenyl substituent at the 2-position. They are both metabolites and nematicides. Flavonoids have been reported in tea (Camellia sinensis), oldenlandia diffusa (Anaphalis lactea), and other organisms with relevant data. Quercetin is a flavonoid compound and forms the "backbone" of many other flavonoids, including citrus flavonoids such as rutin, hesperidin, naringin, and citrus glycoside. Studies have shown that quercetin is the most active flavonoid, and the activity of many medicinal plants is largely attributed to its high quercetin content. Quercetin exhibits significant anti-inflammatory activity because it directly inhibits multiple initial processes of inflammation. For example, it can inhibit the production and release of histamine and other allergic/inflammatory mediators. Furthermore, it possesses potent antioxidant activity and vitamin C-sparing effects.
Flavone (2-Phenyl-4-chromone) is the parent compound of the flavone class of flavonoids, naturally occurring in fruits, vegetables, and herbs (parsley, celery, chamomile). Broad biological activities: antioxidant, anti-inflammatory, antimicrobial, anticancer. Anticancer mechanisms: mitochondrial apoptosis induction, PI3K/AKT/mTOR inhibition, MAPK modulation. Flavone derivatives are investigated as anticancer agents in preclinical models of colon, lung, and other cancers. Flavone itself has limited bioavailability. Not FDA-approved; strictly for research use. |
| Molecular Formula |
C15H10O2
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|---|---|
| Molecular Weight |
222.24
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| Exact Mass |
222.068
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| CAS # |
525-82-6
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| PubChem CID |
10680
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
367.0±42.0 °C at 760 mmHg
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| Melting Point |
100 °C
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| Flash Point |
171.1±21.4 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.635
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| LogP |
3.56
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
326
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)C2=CC(=O)C3=CC=CC=C3O2
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| InChi Key |
VHBFFQKBGNRLFZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10O2/c16-13-10-15(11-6-2-1-3-7-11)17-14-9-5-4-8-12(13)14/h1-10H
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| Chemical Name |
2-phenylchromen-4-one
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~449.96 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.55 mg/mL (20.47 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 45.5 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 (11.25 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 (11.25 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 | 4.4996 mL | 22.4982 mL | 44.9964 mL | |
| 5 mM | 0.8999 mL | 4.4996 mL | 8.9993 mL | |
| 10 mM | 0.4500 mL | 2.2498 mL | 4.4996 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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