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Exemestane Aromatase inhibitor

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

Cat.No.S1196

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

Chemical Structure

Molecular Weight: 296.4

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Opioid Receptor THR PGES 5-alpha Reductase CCK receptor Mineralocorticoid Receptor GHSR SSTR TSH Receptor GNRH Receptor PGDS
Related Products	Fadrozole (CGS16949A) Obacunone (AI3-37934) alpha-Naphthoflavone Aromatase Antibody [H2G4]

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
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
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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	296.4	Formula	C₂₀H₂₄O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	107868-30-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	FCE24304, PNU155971,EXE			Smiles	CC12CCC3C(C1CCC2=O)CC(=C)C4=CC(=O)C=CC34C

Solubility

In vitro
Batch:

DMSO : 54 mg/mL (182.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.950mg/ml (9.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 59 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.425mg/ml (1.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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 ddH₂O, 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.

Mechanism of Action

Features	17-hydroexemestane is the principal metabolite of Exemestane.
Targets/IC₅₀/Ki	Aromatase (human) ^[1] 30 nM Aromatase (rat) ^[1] 40 nM
In vitro	Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. This compound displaces [³H]DHT from rat prostate androgen receptor with IC50 of 0.9 μM. ^[1] This chemical (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] It 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 this compound are incubated with 20 μg of microsomal protein, in the presence of a fixed amount (50 nM) of [³H]A.
In vivo	Exemestane increases lumbar spine BMD by 14.0% in OVX rats at dose of 100 mg/kg. This compound (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] This chemical (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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/8043491/ [2] https://pubmed.ncbi.nlm.nih.gov/17254854/ [3] https://pubmed.ncbi.nlm.nih.gov/17079446/ [4] https://pubmed.ncbi.nlm.nih.gov/15355898/ [5] https://pubmed.ncbi.nlm.nih.gov/8476783/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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