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.
For research use only. We do not sell to patients.
- Purity: 95.49%
- CAS No.: 162558-94-3
- Formula: C25H26O6
- Molecular Weight:422.47
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HER2 |
MEK |
Ras |
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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] |
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.
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.
Chemical Information
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CAS No. 162558-94-3
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Appearance Solid
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Molecular Weight 422.47
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
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)
Purity & Documentation
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Data Sheet (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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 |
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