4H-Chromen-4-one-o-carborane
4H-Chromen-4-one-o-carborane is an estrogen receptor (ER) agonist, with an EC50 of 0.9 μM for ERα and an EC50 of 11.1 μM for ERβ. 4H-Chromen-4-one-o-carborane also acts as an inhibitor of COX-1 and COX-2, with an IC50 of 6.6 μM for COX-1 and an IC50 of 17.7 μM for COX-2.
For research use only. We do not sell to patients.
- CAS No.: 3097646-96-0
- Formula: C11H16B10O2
- Molecular Weight:288.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
4H-Chromen-4-one-o-carborane (compound 1) (up to 100 μM; 48 h) exhibits only weak antiproliferative activity in HepG2 hepatocellular carcinoma cells (IC50 = 69.5 μM), and shows no activity even at the maximum concentration of 100 μM in Raji, Ramos or PC3 cancer cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Raji (lymphoma), Ramos (lymphoma), PC3 (prostate cancer), HepG2 (hepatocellular carcinoma)
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Concentration:up to 100 μM
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Incubation Time:48 h
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Result:Showed negligible antiproliferative activity in Raji, Ramos, and PC3 cell lines, with IC50 values greater than 100 μM for each.
Exhibited weak antiproliferative activity in HepG2 cells, with an IC50 of 69.5 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:athymic mice (male, nu/nu homozygous, 4−6 weeks old)[1]
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Dosage:0.5 mg
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Administration:i.p.; single dose
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Result:Measured boron content as 11.5 μg/g in blood.
Measured boron content as 14.1 μg/g in liver.
Showed lower boron uptake in all other tested organs (brain, bone, heart, kidney, large intestine, lung, muscle, pancreas, small intestine, spleen, stomach, tumor) than blood.
Chemical Information
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CAS No. 3097646-96-0
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Molecular Weight 288.35
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Formula C11H16B10O2
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SMILES
O=C1C=2C=CC=CC2OC=C1C3456[BH]789[BH]%10%11%12[BH]%13%14%15[BH]%10%169[BH]%13%17%18[BH]%14%19%20[BH]%15%11%21[BH]%1276[BH]%21%195[CH]%17%204[BH]%16%1883
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)