| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
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| ln Vitro |
Gossypetin (20–60 μM; 48 hours; KYSE30, KYSE450, and KYSE510 cells) therapy dramatically and dose-dependently reduced the development of anchorage-dependent esophageal cancer cells. Gossypetin significantly prevents esophageal cancer cells from growing anchorage-independently [1]. The administration of 60 μM gossypetin for three hours to KYSE30 and KYSE410 cells significantly reduced p38 activity in a way that was dependent on dose, confirming that gossypetin directly inhibits MKK3 or MKK6 activity [1]. Treatment with gossypetin (20–40 μM; 48 hours; KYSE450 and KYSE510 cells) shortens the S phase and causes dose-dependent G2 phase cell cycle arrest [1]. Treatment of esophageal cancer cells with gossypetin (20–40 μM; 72 hours) causes intrinsic apoptosis in these cells [1].
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| ln Vivo |
Treatment with gossypetin (100 mg/kg; oral; 5 times weekly; for 21 days; severe combined immunodeficient (SCID) female mice) significantly reduced the size of esophageal tumor growth without significant loss of body weight. Gossypetin significantly reduced Ki67 expression. There were no obvious morphological differences between treated or untreated mouse tissues. In the Gossypetin-treated group, the phosphorylation of p38, the direct downstream protein of MKK3/6, was strongly inhibited [1].
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| Cell Assay |
Cell proliferation experiment [1]
Cell Types: KYSE30, KYSE450, KYSE510 Cell Tested Concentrations: 20 μM, 40 μM, 60 μM Incubation Duration: 48 hrs (hours) Experimental Results: The growth of anchorage-dependent esophageal cancer cells was Dramatically inhibited. Western Blot Analysis[1] Cell Types: KYSE30 and KYSE410 ccells Tested Concentrations: 60 μM Incubation Duration: 3 hrs (hours) Experimental Results: p38 activity was strongly inhibited in a dose-dependent manner. Cell cycle analysis[1] Cell Types: KYSE450 and KYSE510 Cell Tested Concentrations: 20 μM, 40 μM Incubation Duration: 48 hrs (hours) Experimental Results: S phase shortened and G2 phase cell cycle arrest was induced in a dose-dependent manner. Apoptosis analysis [1] Cell Types: Esophageal cancer cells Tested Concentrations: 20 μM, 40 μM Incubation Duration: 72 hrs (hours) Experimental Results: Induced apoptosis of esophageal cancer cells. |
| Animal Protocol |
Animal/Disease Models: Severe combined immunodeficiency (SCID) female mice (6-9 weeks old) esophageal cancer tissue injection [1]
Doses: 100 mg/kg Route of Administration: po (po (oral gavage)) 5 times per week; for 21 days Experimental Results: Inhibited the growth of patient-derived esophageal xenograft tumors in an in vivo mouse model. |
| References | |
| Additional Infomation |
Gossypetin is a hexahydroxyflavone having the hydroxy groups placed at the 3-, 3'-, 4'-, 5- 7- and 8-positions. It has a role as a plant metabolite. It is a 7-hydroxyflavonol and a hexahydroxyflavone. It is a conjugate acid of a gossypetin-3-olate and a gossypetin(1-).
Gossypetin has been reported in Sinocrassula indica, Rhododendron latoucheae, and other organisms with data available. See also: Primula veris flower (part of); Larrea tridentata whole (part of). |
| Molecular Formula |
C15H10O8
|
|---|---|
| Molecular Weight |
318.23
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| Exact Mass |
318.038
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| CAS # |
489-35-0
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| PubChem CID |
5280647
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| Appearance |
Light yellow to green yellow solid powder
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| Density |
1.912 g/cm3
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| Boiling Point |
679.3ºC at 760 mmHg
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| Melting Point |
302-304ºC
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| Flash Point |
260.6ºC
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| Vapour Pressure |
4.49E-19mmHg at 25°C
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| Index of Refraction |
1.863
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| LogP |
1.693
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
23
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| Complexity |
518
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YRRAGUMVDQQZIY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10O8/c16-6-2-1-5(3-7(6)17)14-13(22)12(21)10-8(18)4-9(19)11(20)15(10)23-14/h1-4,16-20,22H
|
| Chemical Name |
2-(3,4-dihydroxyphenyl)-3,5,7,8-tetrahydroxychromen-4-one
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| Synonyms |
Gossypetin C.I. 75750 8 hydroxy Quercetin 8-hydroxy QuercetinArticulatidin Equisporol
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1424 mL | 15.7119 mL | 31.4238 mL | |
| 5 mM | 0.6285 mL | 3.1424 mL | 6.2848 mL | |
| 10 mM | 0.3142 mL | 1.5712 mL | 3.1424 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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