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| 100mg |
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Purity: =99.92%
Formononetin (Biochanin B; Flavosil; Formononetol), an O-methylated isoflavone, is a naturally occuring and bioactive flavonoid found in the root of Astragalus membranaceus. This phytoestrogen has strong antioxidant qualities and selectively inhibits the γ-isoform of alcohol dehydrogenase, or ADH γ. It has been demonstrated that formononetin interacts weakly with human estrogen receptors. In mice, formononetin also causes the proliferation of the mammary glands..
| Targets |
FGFR2 (IC50 = 4.31 μM)
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| ln Vitro |
One of the main isoflavone components found in Astragalus membranaceus is formononetin, which has been demonstrated to offer a number of pharmacological advantages. In human air bags, formononetin demonstrates anti-angiogenic activity. In human invoice tents, formononetin also stimulates cell cycle signaling via Akt/cyclin D1/CDK4 [1]. Significant reduction of FGF2-stimulated endothelial cell proliferation is observed with formononetin (25-150 μM) [1].
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| ln Vivo |
The group treated with formononetin showed a substantial rise in tumor volume and a significant decrease in tumor weight when compared to the vehicle group. There was no discernible weight difference between the excipient group and the formononetin-treated group, and the treatment with formononetin was well tolerated [1].
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| Enzyme Assay |
FGFR2 kinase inhibition assay [1]
The IC50 values for inhibition of FGFR2 by formononetin was determined using a FRET-based in vitro kinase assay (Z'-lyte assay). The kinase domains of FGFR2 was assayed in 50 mm HEPES pH 7.5, 0.01% BRIJ-35, 10 mm MgCl2, 2 mm MnCl2, 1 mm EGTA, 1 mm DTT, with 20 μm or 80 μm ATP, respectively. The assay was performed in triplicate in 384-well plates according to the manufacturer's instructions |
| Cell Assay |
Cell viability assay [1]
Cell Types: HUVEC Tested Concentrations: 0, 10, 25, 50, 75, 100 and 150 μM Incubation Duration: Experimental Results: Dramatically diminished the proliferation of FGF2-stimulated HUVEC in a dose-dependent manner, while the proliferation of HUVEC not stimulated by FGF2 was Dramatically diminished. Stimulated HUVEC had little inhibitory effect. |
| Animal Protocol |
Animal/Disease Models: BALB/c nude mice carrying MDA-MB-231 xenografts [1]
Doses: 100 mg/kg Route of Administration: Daily intragastric (po) (po)administration for 25 days Experimental Results: Inhibition of breast cancer growth and blood vessels in vivo generate. |
| References |
[1]. Xiao Yu Wu,et al. Formononetin, a novel FGFR2 inhibitor, potently inhibits angiogenesis and tumor growth in preclinical models. Oncotarget. 2015 Dec 29;6(42):44563-78.
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| Molecular Formula |
C16H12O4
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| Molecular Weight |
268.27
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| Exact Mass |
268.07
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| Elemental Analysis |
C, 71.64; H, 4.51; O, 23.86
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| CAS # |
485-72-3
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| Related CAS # |
Formononetin-d3-1
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| Appearance |
Solid powder
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| Source |
Isoflavones from Astragalus membranaceus
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| LogP |
2.8
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| tPSA |
55.8Ų
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| SMILES |
COC1=CC=C(C=C1)C2=COC3=C(C2=O)C=CC(=C3)O
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| InChi Key |
HKQYGTCOTHHOMP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12O4/c1-19-12-5-2-10(3-6-12)14-9-20-15-8-11(17)4-7-13(15)16(14)18/h2-9,17H,1H3
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| Chemical Name |
7-hydroxy-3-(4-methoxyphenyl)chromen-4-one
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.32 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 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 (9.32 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (9.32 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 | 3.7276 mL | 18.6379 mL | 37.2759 mL | |
| 5 mM | 0.7455 mL | 3.7276 mL | 7.4552 mL | |
| 10 mM | 0.3728 mL | 1.8638 mL | 3.7276 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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