Name: Exemestane
Brand: Selleck Chemicals
SKU: S1196
Rating: 5 (22 reviews)

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

Exemestane Chemical Structure

CAS: 107868-30-4

Selleck's Exemestane has been cited by 22 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.96%

99.96

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Signaling Pathway

Aromatase Signaling Pathway

Choose Selective Aromatase Inhibitors

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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
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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
Kinase Assay	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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 ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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