| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
- 3',4',5',5,7-Pentamethoxyflavone targets the Nrf2 (nuclear factor erythroid 2-related factor 2) signaling pathway, inhibiting Nrf2 nuclear translocation and downstream gene expression [1]
|
|---|---|
| ln Vitro |
- In cisplatin-resistant A549 (A549/DDP) cells:
1. CCK-8 assay: 3',4',5',5,7-Pentamethoxyflavone alone (10 μM, 20 μM) for 48 hours had <10% cell viability inhibition. Combined with cisplatin, it reduced cisplatin’s IC50 from 28.5 μM (alone) to 18.7 μM (10 μM flavone + cisplatin) and 12.3 μM (20 μM flavone + cisplatin) [1] 2. Annexin V-FITC/PI staining: 20 μM flavone + 20 μM cisplatin induced 38.6% apoptosis, higher than cisplatin alone (12.4%) or flavone alone (4.2%) [1] 3. Western blot & qPCR: 10 μM, 20 μM flavone reduced Nrf2 nuclear translocation by 35%/58%, and lowered HO-1/NQO1 (Nrf2 targets) protein (28%-45%) and mRNA (32%-51%) expression [1] 4. Colony formation assay: 20 μM flavone + 15 μM cisplatin decreased colony number by 72% vs. cisplatin alone [1] |
| Cell Assay |
- CCK-8 assay: A549/DDP cells (5×10³/well) were treated with flavone (10/20 μM), cisplatin (5-40 μM), or combinations for 48 hours. CCK-8 solution was added, absorbance measured at 450 nm to calculate viability and cisplatin IC50 [1]
- Apoptosis assay: Cells (2×10⁵/well) were treated for 48 hours, stained with Annexin V-FITC/PI, and apoptotic rate analyzed by flow cytometry [1] - Nrf2 pathway detection: Cells (5×10⁶) were treated for 24 hours. Nuclear/cytoplasmic proteins were extracted for Western blot (Nrf2, HO-1, NQO1); total RNA was used for qPCR to measure HO-1/NQO1 mRNA (2⁻ΔΔCt method) [1] - Colony formation assay: Cells (500/well) were treated for 24 hours, cultured for 14 days, fixed with methanol, stained with crystal violet, and colonies >50 cells counted [1] |
| References | |
| Additional Infomation |
It has been reported that 3',4',5',5,7-pentamethoxyflavone exists in Ficus formosana, Cedera, and other organisms with relevant data. 3',4',5',5,7-pentamethoxyflavone is a natural flavonoid derivative [1] It sensitizes A549/DDP cells to cisplatin by inhibiting Nrf2 nuclear translocation, reducing HO-1/NQO1 expression, increasing intracellular cisplatin accumulation and oxidative stress, and promoting apoptosis [1].
|
| Molecular Formula |
C20H20O7
|
|---|---|
| Molecular Weight |
372.3686
|
| Exact Mass |
372.121
|
| CAS # |
53350-26-8
|
| PubChem CID |
493376
|
| Appearance |
White to off-white solid powder
|
| Density |
1.244g/cm3
|
| Boiling Point |
554.4ºC at 760mmHg
|
| Melting Point |
198-200ºC
|
| Flash Point |
243.5ºC
|
| Index of Refraction |
1.565
|
| LogP |
3.503
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
27
|
| Complexity |
534
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
GIKVSFNAEBQLGB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H20O7/c1-22-12-8-15(23-2)19-13(21)10-14(27-16(19)9-12)11-6-17(24-3)20(26-5)18(7-11)25-4/h6-10H,1-5H3
|
| Chemical Name |
5,7-dimethoxy-2-(3,4,5-trimethoxyphenyl)chromen-4-one
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~20 mg/mL (~53.71 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6855 mL | 13.4275 mL | 26.8550 mL | |
| 5 mM | 0.5371 mL | 2.6855 mL | 5.3710 mL | |
| 10 mM | 0.2686 mL | 1.3428 mL | 2.6855 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.