Broussoflavonol F
Based on 1 Customer Validation
Broussoflavonol F is a potent dual inhibitor of the HER2-RAS-MEK-ERK signaling pathway and mushroom tyrosinase with an IC50 value of 82.3 μM. Broussoflavonol F downregulates the expression of RAS, HER2, phosphorylated BRAF, phosphorylated MEK and phosphorylated Erk proteins. Broussoflavonol F induces cell cycle arrest and apoptosis, and exhibits cytotoxicity in colon cancer cells. Broussoflavonol F inhibits endothelial proliferation, migration and tube formation, suppresses subintestinal vascular development, and reduces the mRNA levels of angiogenesis-associated genes.Broussoflavonol F can be used for colon cancer research.
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- Pureté : 95.49%
- CAS No.: 162558-94-3
- Formule: C25H26O6
- Masse moléculaire:422.47
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Stockage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
HER2 |
MEK |
Ras |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hep 3B2 | IC50 |
1.15 μM
Compound: 21
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Cytotoxicity against human Hep3B cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
Cytotoxicity against human Hep3B cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
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[PMID: 36549116] |
| HepG2 | IC50 |
30.79 μM
Compound: 21
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Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
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[PMID: 36549116] |
| Platelet | IC50 |
16.9 μM
Compound: 16
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Antiplatelet activity against rabbit platelets assessed as arachidonic acid-induced platelet aggregation by turbidimetric method
Antiplatelet activity against rabbit platelets assessed as arachidonic acid-induced platelet aggregation by turbidimetric method
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[PMID: 8864236] |
| Platelet | IC50 |
2.7 μM
Compound: 6
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Antiplatelet activity against rabbit platelet assessed as inhibition of platelet-activating factor-induced platelet aggregation at 20 uM preincubated 3 mins before PAF challenge by turbidimetric method relative to control
Antiplatelet activity against rabbit platelet assessed as inhibition of platelet-activating factor-induced platelet aggregation at 20 uM preincubated 3 mins before PAF challenge by turbidimetric method relative to control
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[PMID: 9358644] |
In Vitro
Broussoflavonol F (BFF) (0-20 μM; 24-48 h) exerts selective, concentration- and time-dependent cytotoxicity against HCT-116, LoVo, HT-29, SW480, and colon 26 colon cancer cells, with IC50 values of 6.64 μM (HCT-116) and 7.37 μM (LoVo) after 48 h, and is far less cytotoxic to PBMCs (IC50 = 47 μM)[1].
Broussoflavonol F (1.25-7.5 μM (HCT-116); 2.5-10 μM (LoVo); 24-48 h) effectively suppresses colony formation in HCT-116 and LoVo colon cancer cells after 24 h and 48 h treatment[1].
Broussoflavonol F (1.25-5 μM; 24-48 h) induces G0/G1 phase cell cycle arrest and reduces G2/M phase cell numbers in HCT-116 and LoVo colon cancer cells[1].
Broussoflavonol F (2.5-7.5 μM (HCT-116); 5-10 μM (LoVo); 24-48 h) significantly increases apoptosis in HCT-116 and LoVo colon cancer cells[1].
Broussoflavonol F (1.25-5 μM; 24-48 h) downregulates HER2, RAS, p-BRAF, p-MEK, and p-Erk protein expression (without altering total BRAF, MEK, or Erk) in HCT-116 and LoVo colon cancer cells after 24 h and 48 h treatment, inhibiting the HER2-RAS-MEK-ERK pathway[1].
Broussoflavonol F (0-20 μM; 48 h) exhibits cytotoxicity to HMEC-1 cells with an IC50 of 7.1 μM after 48 h treatment[1].
Broussoflavonol F (40 μM; 6 h) inhibits tube formation in HMEC-1 cells after 6 h incubation[1].
Broussoflavonol F (5 μM; 24 h) reduces cell motility in HMEC-1 cells after 24 h treatment[1].
Broussoflavonol F inhibits mushroom tyrosinase using L-tyrosine as substrate with an IC50 of 388.6 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human colon cancer HCT-116 and LoVo cells
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Concentration:2.5, 5, 7.5, 10 μM
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Incubation Time:24 h; 48 h
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Result:Effectively suppressed colony formation in both HCT-116 and LoVo cells after 24 h and 48 h treatment.
Exhibited suppressive effects similar to the positive control 5-FU at 5 μM (HCT-116) and 7.5 μM (LoVo).
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Cell Line:human colon cancer HCT-116 and LoVo cells
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Concentration:1.25-5 μM
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Incubation Time:24 h; 48 h
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Result:Significantly arrested cells at the G0/G1 phase, accompanied by a decrease in cell number in the G2/M phase in both HCT-116 and LoVo cells after 24 h and 48 h incubation.
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Cell Line:human colon cancer HCT-116 and LoVo cells
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Concentration:2.5, 5, 7.5 μM (HCT-116); 5, 7.5, 10 μM (LoVo)
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Incubation Time:24 h; 48 h
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Result:Effectively increased the percentage of apoptotic cells in both HCT-116 and LoVo cells after 24 h and 48 h treatment.
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Cell Line:human colon cancer HCT-116 and LoVo cells
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Concentration:1.25, 2.5, 5 μM
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Incubation Time:24 h; 48 h
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Result:Significantly decreased the expression levels of HER2, RAS, p-BRAF, p-MEK, and p-Erk in both HCT-116 and LoVo cells after 24 h and 48 h treatment.
Did not regulate the expression levels of total BRAF, MEK, and Erk proteins.
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Cell Line:human microvascular endothelial HMEC-1 cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Significantly decreased cell motility after 24 h treatment.
In Vivo
Broussoflavonol F (5-10 mg/kg; i.p.; daily; 21 days) at 10 mg/kg suppresses in vivo colon tumor growth, reduces tumor cell proliferation and angiogenesis, and downregulates the HER2-RAS-MEK-ERK pathway in HCT116 xenograft-bearing mice without inducing measurable liver or muscle toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tg(fli1:EGFP)y1 transgenic line (24 hours post-fertilization embryos)[1]
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Dosage:1.25 µM, 2.5 µM, 5 µM
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Administration:immersion; continuous; 48 hours
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Result:Significantly reduced the length of subintestinal vessels (SIVs) in a concentration-dependent manner at 2.5 µM and 5 µM (p < 0.0001).
Significantly suppressed mRNA expressions of angiogenesis-related genes NRP1a, PDGFba, PDGFRb, KDR, and FLT1 at 5 µM.
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Animal Model:Male nude mice (6-8 weeks old, 25-30 g; subcutaneous xenograft of human HCT116 colon cancer cells)[1]
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Dosage:5 mg/kg, 10 mg/kg
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Administration:i.p.; daily; 21 days
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Result:Significantly reduced final tumor weight relative to control at 10 mg/kg.
Downregulated tumor tissue expressions of RAS, p-BRAF, p-MEK, and p-Erk proteins at 5 mg/kg and 10 mg/kg.
Decreased the number of Ki-67-positive (proliferation) and CD31-positive (angiogenesis) cells in tumor sections at 10 mg/kg.
Caused no significant changes in plasma alanine aminotransferase (ALT), aspartate aminotransferase (AST), creatine kinase (CK), or lactate dehydrogenase (LDH) levels, indicating no obvious liver or muscle toxicity.
- RNA extraction experimental
- Human pluripotent stem cell endothelial-cell differentiation
- Mammalian live/dead viability and cytotoxicity staining
- Vascular/Branching Fractal Analysis
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Cell migration
- Protocol for Cell Cycle
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Cell Cytotoxicity Assay
- Endothelial Tube Formation Assay
- Apoptosis Solutions
- Endothelial Cell Migration/Angiogenic Sprouting Assay
Chemical Information
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CAS No. 162558-94-3
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Appearance Solid
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Masse moléculaire 422.47
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Formule C25H26O6
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Color Light yellow to yellow
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SMILES
O=C1C(O)=C(C2=CC=C(O)C(C/C=C(C)\C)=C2)OC3=C(C/C=C(C)\C)C(O)=CC(O)=C13
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (236.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Pureté et documentation
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Fiche technique (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3670 mL | 11.8352 mL | 23.6703 mL | 59.1758 mL |
| 5 mM | 0.4734 mL | 2.3670 mL | 4.7341 mL | 11.8352 mL | |
| 10 mM | 0.2367 mL | 1.1835 mL | 2.3670 mL | 5.9176 mL | |
| 15 mM | 0.1578 mL | 0.7890 mL | 1.5780 mL | 3.9451 mL | |
| 20 mM | 0.1184 mL | 0.5918 mL | 1.1835 mL | 2.9588 mL | |
| 25 mM | 0.0947 mL | 0.4734 mL | 0.9468 mL | 2.3670 mL | |
| 30 mM | 0.0789 mL | 0.3945 mL | 0.7890 mL | 1.9725 mL | |
| 40 mM | 0.0592 mL | 0.2959 mL | 0.5918 mL | 1.4794 mL | |
| 50 mM | 0.0473 mL | 0.2367 mL | 0.4734 mL | 1.1835 mL | |
| 60 mM | 0.0395 mL | 0.1973 mL | 0.3945 mL | 0.9863 mL | |
| 80 mM | 0.0296 mL | 0.1479 mL | 0.2959 mL | 0.7397 mL | |
| 100 mM | 0.0237 mL | 0.1184 mL | 0.2367 mL | 0.5918 mL |
Broussoflavonol F Related Classifications
HY-N9330 Related Classifications
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Keywords
- Broussoflavonol F
- 162558-94-3
- Xanthine Oxidase
- Ras
- EGFR
- MEK
- PERK
- Apoptosis
- XO
- Epidermal growth factor receptor
- ErbB-1
- HER1
- Mitogen-activated protein kinase kinase
- MAPKK
- MAP2K
- Protein kinase R-like endoplasmic reticulum kinase
- PKR-like endoplasmic reticulum kinase
- colon cancer cells
- mushroom tyrosinase
- SW480
- PBMCs
- HT-29
- HMEC-1
- HER2-RAS-MEK-ERK signaling pathway
- HCT-116
- LoVo
- colon 26
- Inhibitor
- inhibitor
- inhibit