Casimiroin
Casimiroin is a QR2 and Aromatase inhibitor, with an IC50 of 54.1 μM against QR2 and an IC50 of 3.92 μM against aromatase. Casimiroin exhibits antimutagenic activity and inhibits DMBA (HY-W011845)-induced mutations in Salmonella typhimurium. Casimiroin suppresses DMBA-induced precancerous lesions in mouse mammary organ cultures. Casimiroin can be used in breast cancer-related research.
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- CAS No.: 477-89-4
- Formule: C12H11NO4
- Masse moléculaire:233.22
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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Aromatase 3.92 μM (IC50) |
QR2 54.1 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
>85.81 μM
Compound: 1
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Cytotoxicity against human LNCAP cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human LNCAP cells after 72 hrs by sulforhodamine B assay
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[PMID: 19265439] |
| MCF7 | IC50 |
>85.81 μM
Compound: 1
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Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay
Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay
|
[PMID: 19265439] |
Casimiroin (0.4-500 μM) inhibits purified human QR2 with an IC50 of 54.1 μM[1].
Casimiroin (range of concentrations; 10 min preincubation; 30 min enzyme incubation; 2 h post-quench incubation) inhibits recombinant aromatase (CYP19) with an IC50 of 3.92 μM[1].
Casimiroin (0-20 μg/mL; 72 h) is not cytotoxic to Hepa 1c1c7, MCF7, LNCaP, or LU cell lines, with IC50 values >85.81 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hepa 1c1c7 (mouse liver), MCF7 (breast), LNCaP (prostate), LU (lung)
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Concentration:0-20 μg/mL
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Incubation Time:72 h
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Result:Showed no significant cytotoxicity in any of the four cell lines, with IC50 values greater than 85.81 μM for all tested cell lines.
Chemical Information
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CAS No. 477-89-4
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Masse moléculaire 233.22
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Formule C12H11NO4
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SMILES
O=C1C=C(OC)C=2C=CC=3OCOC3C2N1C
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Maiti A, et al. Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities. Journal of medicinal chemistry. 2009 Apr 09;52(7):1873-84. [Content Brief]
[2]. Wang M, et al. Synthesis of carbon-11-labeled casimiroin analogues as new potential PET agents for imaging of quinone reductase 2 and aromatase expression in breast cancer. Steroids. 2010 Dec;75(12):967-73. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)