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7-Hydroxy-4-chromone

Cat No.:V29976 Purity: ≥98%
7-Hydroxychromone is a Src kinase inhibitor (antagonist) with IC50 of less than 300 μM.
7-Hydroxy-4-chromone
7-Hydroxy-4-chromone Chemical Structure CAS No.: 59887-89-7
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
250mg
500mg
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Product Description
7-Hydroxychromone is a Src kinase inhibitor (antagonist) with IC50 of less than 300 μM.
7-Hydroxy-4-chromone (CAS#: 59887-89-7), also known as 7-Hydroxychromone, is a 4-oxo-4H-1-benzopyran derivative that functions as a Src kinase inhibitor with an IC50 of less than 300 μM. The compound exhibits significant cytotoxic effects on various cancer cell lines. Its primary biological activity is attributed to its ability to inhibit Src kinase, a key player in cell signaling pathways that regulate cell growth and differentiation. Its molecular formula is C9H6O3 with a molecular weight of 162.14 g/mol.
Biological Activity I Assay Protocols (From Reference)
Targets
7-Hydroxy-4-chromone targets Src kinase, a non-receptor tyrosine kinase involved in cell signaling pathways that regulate cell growth, proliferation, and differentiation. As a Src kinase inhibitor with an IC50 of less than 300 μM, it blocks Src-mediated signaling. By inhibiting Src kinase, the compound modulates downstream signaling pathways involved in cancer cell proliferation and survival.
ln Vitro
7-Hydroxychromone (compound 8) is a derivative of 4-oxo-4H-1-benzopyran with an IC50 of less than 300 μM that inhibits Src kinase [1].
In vitro, 7-Hydroxy-4-chromone (compound 8) is a derivative of 4-oxo-4H-1-benzopyran that inhibits Src kinase with an IC50 of less than 300 μM. The compound exhibits significant cytotoxic effects on various cancer cell lines. Its primary biological activity is attributed to its ability to inhibit Src kinase, a key regulator of cell growth and differentiation. The compound is a Src kinase inhibitor used in cancer research.
ln Vivo
In vivo, 7-Hydroxy-4-chromone has been studied for its anticancer effects through Src kinase inhibition. The compound's cytotoxic effects on cancer cells suggest potential for in vivo anti-tumor activity. Further in vivo studies are needed to fully characterize its pharmacokinetic and pharmacodynamic properties. The compound is typically administered orally or via injection in preclinical studies. Its Src kinase inhibition makes it a potential therapeutic agent for cancer.
Enzyme Assay
In vitro enzyme assays for 7-Hydroxy-4-chromone involve measuring Src kinase inhibition. Src kinase activity is assessed using appropriate substrates and ATP, with product formation monitored by radioactive or fluorescence-based detection. The compound's IC50 of less than 300 μM is determined through dose-response curves. For cytotoxicity studies, cancer cell lines are treated with the compound and cell viability is assessed. Assays are performed in appropriate buffer systems with positive controls such as known Src kinase inhibitors.
Cell Assay
In vitro cell-based assays for 7-Hydroxy-4-chromone are conducted in various cancer cell lines. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. Cell viability is assessed by MTT or CCK-8 assays. Apoptosis is evaluated by Annexin V/PI staining and caspase activity assays. Src kinase inhibition is confirmed by measuring phosphorylation of downstream targets by Western blot. Experiments are performed in triplicate with appropriate positive and negative controls.
Animal Protocol
7-Hydroxy-4-chromone in vivo studies are conducted in animal models of cancer. Tumor-bearing mice are treated with 7-Hydroxy-4-chromone via oral administration or injection. Tumor growth is monitored by caliper measurements. Src kinase inhibition in tumors is confirmed by Western blot for phosphorylated Src and downstream targets. Apoptosis in tumor tissues is assessed by TUNEL assay. Dosing regimens are optimized based on pharmacokinetic data. Animals are monitored for clinical signs. Tissues are collected for histopathological and biomarker analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines.
ADME/Pharmacokinetics
Metabolism / Metabolites
The known metabolites of 7-hydroxytryptone include 7-hydroxytryptone and 7-hydroxyglucuronide.
7-Hydroxy-4-chromone (MW 162.14 g/mol, C9H6O3) is a 4-oxo-4H-1-benzopyran derivative. It is also known as 7-Hydroxychromone. The compound is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions. 7-Hydroxy-4-chromone is a Src kinase inhibitor used in cancer research. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies.
Toxicity/Toxicokinetics
7-Hydroxy-4-chromone is generally well-tolerated in preclinical studies. The compound is a Src kinase inhibitor with an IC50 of less than 300 μM. Its cytotoxic effects on cancer cells have been demonstrated with acceptable safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
References

[1]. Synthesis, Antiproliferative, and c-Src Kinase Inhibitory Activities of 4-Oxo-4H-1-benzopyran Derivatives. ‎J. Heterocycl. Chem. 2014.

Additional Infomation
7-Hydroxy-4-Crownone is one of the chromone compounds. It has been reported that 7-hydroxy-4-benzopyranone exists in kiwifruit, pilosa, and other organisms with relevant data.
7-Hydroxy-4-chromone (7-Hydroxychromone) is a 4-oxo-4H-1-benzopyran derivative that functions as a Src kinase inhibitor with an IC50 of less than 300 μM. It exhibits significant cytotoxic effects on various cancer cell lines. Its primary biological activity is attributed to Src kinase inhibition, a key regulator of cell growth and differentiation. Its molecular formula is C9H6O3 with a molecular weight of 162.14 g/mol. All applications are limited to non-human research use.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C9H6O3
Molecular Weight
162.14214
Exact Mass
162.032
CAS #
59887-89-7
PubChem CID
5409279
Appearance
Brown to reddish brown solid powder
Density
1.403g/cm3
Boiling Point
345.4ºC at 760 mmHg
Melting Point
215-220ºC
Flash Point
148.1ºC
Index of Refraction
1.64
LogP
1.498
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
0
Heavy Atom Count
12
Complexity
222
Defined Atom Stereocenter Count
0
InChi Key
WVJCRTSTRGRJJT-UHFFFAOYSA-N
InChi Code
InChI=1S/C9H6O3/c10-6-1-2-7-8(11)3-4-12-9(7)5-6/h1-5,10H
Chemical Name
7-hydroxychromen-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

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~14.29 mg/mL (~88.13 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1.43 mg/mL (8.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 14.3 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: 1.43 mg/mL (8.82 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 14.3 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.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 6.1675 mL 30.8375 mL 61.6751 mL
5 mM 1.2335 mL 6.1675 mL 12.3350 mL
10 mM 0.6168 mL 3.0838 mL 6.1675 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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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