Home Endocrinology & Hormones Aromatase inhibitor Exemestane For research use only.

Exemestane

Synonyms: FCE24304, PNU155971,EXE

Exemestane is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.

Exemestane Chemical Structure

Exemestane Chemical Structure

CAS No. 107868-30-4

Purity & Quality Control

Exemestane Related Products

Signaling Pathway

Aromatase Signaling Pathways

Aromatase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF7a cells Cytotoxicity assay 10 days Cytotoxicity against human MCF7a cells expressing Tet-off-3betaHSD1-Arom assessed as inhibition of TST-stimulated cell proliferation measured after 10 days, EC50=5.6 nM 22951074
human MCF7 cells Cytotoxicity assay 10 to 15 μM 3-6 days Cytotoxicity against human placental microsome aromatase expressing human MCF7 cells assessed as reduction in cell viability at 10 to 15 uM after 3 to 6 days by MTT assay in presence of estradiol 25277066
Click to View More Cell Line Experimental Data

Biological Activity

Description Exemestane is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
Features 17-hydroexemestane is the principal metabolite of Exemestane.
Targets
Aromatase (human) [1] Aromatase (rat) [1]
30 nM 40 nM
In vitro
In vitro

Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. Exemestane displaces [3H]DHT from rat prostate androgen receptor with IC50 of 0.9 μM. [1] Exemestane (1 μM) increases alkaline phosphatase activity in hFOB and Saos-2 cells and induces the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and glypican 2 in hFOB cells. [2] Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells. [3]
Kinase Assay Assays with human placental aromatase
Microsomes are prepared from human placenta and stored at -80℃. The rate of aromatization is determined by measuring the tritiated water released from [1β-3H]A. The assay is carried out in a final volume of 1 mL, in 10 mM phosphate buffer, pH 7.5, containing 100 mM KCl, 1 mM EDTA, 1 mM dithiothreitol, 100 μM NADPH, the enzyme preparation and the appropriate concentrations of Exemestane (in duplicate) and the substrate. After a 10 min incubation at 37 ℃, the assay is terminated by the addition of 4 mL cold chloroform. The acqueous phase is treated with a charcoal suspension, the supernatant is removed and counted for radioactivity by liquid scintillation in Rialuma. For the determination of the IC50 values, various concentrations of Exemestane are incubated with 20 μg of microsomal protein, in the presence of a fixed amount (50 nM) of [3H]A.
Cell Research Cell lines hFOB cells
Concentrations 1 μM
Incubation Time 24 hours
Method

hFOB is treated with steroids and Exemestane for 24 hours, when specimens are harvested and evaluated for cell proliferation using the WST-8 method. Optical densities (OD, 450 nm) are evaluated using a SpectraMax 190 microplate reader and Softmax Pro 4.3 microplate analysis software. The status of proliferation (%) is calculated according to the following equation: (cell OD value after test materials treated /vehicle control cell OD value)× 10
In Vivo
In vivo

Exemestane increases lumbar spine BMD by 14.0% in OVX rats at dose of 100 mg/kg. Exemestane (100 mg/kg) and 17-hydroexemestane (20 mg/kg) significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin in rats and causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol inOVX rats. [4] Exemestane (20 mg/kg/day s.c.) induces 26% complete (CR) and 18% partial (PR) tumor regressions in rats with 7,12-dimethylbenzanthracene (DMBA)-induced mammary tumors. [5]
Animal Research Animal Models estrogen-deficient ovariectomized (OVX) rats
Dosages 100 mg/kg
Administration Intramuscular injection
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06288412 Recruiting
Diabetes Mellitus Type 2
Novo Nordisk A/S
 February 26 2024 Phase 1
NCT06379282 Recruiting
Chronic Lymphocytic Leukemia|Frailty|Muscle Function|Immune Function|Lipid Cell; Tumor
University of Surrey|American Society of Hematology
 October 14 2022 Not Applicable
NCT04296565 Recruiting
Mild Cognitive Impairment
VA Office of Research and Development
 January 3 2022 Phase 4
NCT04692909 Unknown status
Food Addiction|Obesity Morbid
Soroka University Medical Center
 January 15 2021 Not Applicable
NCT04572295 Active not recruiting
Breast Neoplasms
Eisai Co. Ltd.|Eisai Inc.
 October 9 2020 Phase 1

Chemical Information & Solubility

Molecular Weight 296.4 Formula

C20H24O2
CAS No. 107868-30-4 SDF Download Exemestane SDF
Smiles CC12CCC3C(C1CCC2=O)CC(=C)C4=CC(=O)C=CC34C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 54 mg/mL ( (182.18 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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