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Exemestane

Name: Exemestane
Brand: TargetMol
SKU: T1587
Price: 50 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1587Cas No. 107868-30-4

Alias PNU155971, FCE 24304, EXE

Exemestane (EXE) is an Aromatase Inhibitor. The mechanism of action of exemestane is as an Aromatase Inhibitor.

Exemestane

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Purity: 99.35%

Catalog No. T1587Alias PNU155971, FCE 24304, EXECas No. 107868-30-4

Exemestane (EXE) is an Aromatase Inhibitor. The mechanism of action of exemestane is as an Aromatase Inhibitor.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mL x 10 mM (in DMSO)	$50	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:99.35%

Color:White

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COA HNMR HPLC LCMS

Product Introduction

Bioactivity

Description	Exemestane (EXE) is an Aromatase Inhibitor. The mechanism of action of exemestane is as an Aromatase Inhibitor.
Targets&IC50	Aromatase (rat):40 nM, Aromatase (human):30 nM
In vitro	Exemestane (1 μM) increased alkaline phosphatase activity in hFOB and Saos-2 cells and induced the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and phosphatidylinositol proteoglycan 2 in hFOB cells.Exemestane competitively inhibited and time-dependently inactivated human placenta at Ki 4.3 nM. Exemestane substituted for [3 H] DHT at the rat prostate androgen receptor with an IC50 of 0.9 μM.Exemestane induced aromatase degradation in MCF-7aro cells in a dose-responsive manner.
In vivo	Exemestane (1 μM) increased alkaline phosphatase activity in hFOB and Saos-2 cells and induced the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and phosphatidylinositol proteoglycan 2 in hFOB cells.Exemestane competitively inhibited and time-dependently inactivated human placenta at Ki 4.3 nM. Exemestane substituted for [3 H] DHT at the rat prostate androgen receptor with an IC50 of 0.9 μM.Exemestane induced aromatase degradation in MCF-7aro cells in a dose-responsive manner.
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	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(Only for Reference)
Synonyms	PNU155971, FCE 24304, EXE

Chemical Properties

Molecular Weight	296.4
Formula	C₂₀H₂₄O₂
Cas No.	107868-30-4
Smiles	C[C@]12CCC3C(CC(=C)C4=CC(=O)C=C[C@]34C)C1CCC2=O
Relative Density.	1.13 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 2.97 mg/mL (10.02 mM), Sonication is recommended.

Ethanol: 22.2 mg/mL (74.9 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (3.37 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	3.3738 mL	16.8691 mL	33.7382 mL	168.6910 mL
5 mM	0.6748 mL	3.3738 mL	6.7476 mL	33.7382 mL
10 mM	0.3374 mL	1.6869 mL	3.3738 mL	16.8691 mL

Ethanol

	1mg	5mg	10mg	50mg
20 mM	0.1687 mL	0.8435 mL	1.6869 mL	8.4345 mL
50 mM	0.0675 mL	0.3374 mL	0.6748 mL	3.3738 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc