Exemestane (Synonyms: Aromasin, FCE 24304) |
Catalog No.GC11813
One-Click Copy Product Info
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L'exémestane (FCE 24304) est un inhibiteur de l'aromatase stéroÏdienne sélectif, irréversible et actif par voie orale avec des CI50 de 30 nM et 40 nM pour l'aromatase placentaire humaine et ovarienne de rat, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 107868-30-4
Sample solution is provided at 25 µL, 10mM.
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Exemestane is a novel selective and irreversible aromatase inhibitor with an IC50 value of 27 nM. The human placental aromatase was proved to be inhibited by exemestane with Ki of 26 nM and t1/2 of 13.9 min.[1]
Aromatase is a cytochrome P450 enzyme, catalyzing the transformation from androgens to estrogen.[2] Structurally similar to androstenedione, exemestane might have a big impact on androgenic effect. Exemestane can irreversibly inactivate aromatase by interacting with the substrate binding site on the peptide moiety of the enzyme. After binding to the active site, it will be converted to an intermediate that covalently binds to the aromatase binding site, rendering the enzyme inactive. Exemestane has been proved to inhibit aromatase activity in human placental microsomes in-vitro, besides, it can inhibit aromatase activity in the cultured tissue fibroblasts and breast cancer specimens as well. On the other hand, exemestane has been suggested to affect the blood levels and urinary estrogens in-vivo.[3]
References:
[1] Franco Buzzetti, Enrico Di Salle, Antonio Longo, Gabriella Briatico. Synthesis and aromatase inhibition by potential metabolites of exemestane (6-methylenandrosta-1,4-diene-3,17-dione). Steroids. November 1993. 58(11): 527-532.
[2] Gustavo de Albuquerque Cavalcanti, Bruno Carius Garrido, Felipe Dias Leal, Monica Costa Padilha, Xavier de la Torre, Francisco Radler de Aquino Neto. Detection of new urinary exemestane metabolites by gas chromatography coupled to mass spectrometry. Steroids. September–October 2011. 76(10-11): 1010-1015.
[3] Stephanie A. Jones, Stephen E. Jones. Exemestane: A Novel Aromatase Inactivator for Breast Cancer. Clinical Breast Cancer. October 2000. 1(3): 211-216.
| Cas No. | 107868-30-4 | SDF | |
| Synonymes | Aromasin, FCE 24304 | ||
| Chemical Name | (8R,9S,10R,13S,14S)-10,13-dimethyl-6-methylidene-7,8,9,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-3,17-dione | ||
| Canonical SMILES | CC12CCC3C(C1CCC2=O)CC(=C)C4=CC(=O)C=CC34C | ||
| Formula | C20H24O2 | M.Wt | 296.4 |
| Solubility | ≥ 14.82mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3738 mL | 16.8691 mL | 33.7382 mL |
| 5 mM | 674.8 μL | 3.3738 mL | 6.7476 mL |
| 10 mM | 337.4 μL | 1.6869 mL | 3.3738 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)