Exemestane

Licensed by Pfizer Catalog No.S1196 Synonyms: FCE24304, PNU155971

Exemestane Chemical Structure

Molecular Weight(MW): 296.4

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

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 150 In stock
USD 270 In stock
USD 470 In stock
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2 Customer Reviews

  • Effect of exemestane on phosphatidylserine exposure. A. Original histogram of annexin-V-binding of erythrocytes following exposure for 48 hours to Ringer solution without (grey area) and with (black line) presence of 40 µg/ml exemestane. B. Arithmetic means ± SEM (n = 24) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) exemestane (10-40 µg/ml). For comparison, the effect of the solvent DMSO is shown (grey bar). **(p<0.01),***(p<0.001) indicates significant difference from the absence of exemestane (ANOVA).

    Cell Physiol Biochem, 2017, 42(1):1-12. Exemestane purchased from Selleck.

    Expression of ER, PR, Bcl-2, HER receptors and CYP19A1 mRNA in MCF-7 and AI-resistant cell lines. (A) Western blot analysis of lysates from MCF-7 cells grown with 10% NCS+10-7 M testosterone (MCF-7) and LetR-1, LetR-3, ExeR-1 and ExeR-3 grown in their standard growth medium with 10-6 M letrozole and 10-7 M exemestane, respectively. β-actin and Hsp70 were used as loading controls. (B) Western blot analysis of lysates from MCF-7, LetR-1 and ExeR-1 cells grown for five days in 10% NCS (C) or 10% NCS + 10-12 M estradiol (E2), 10% NCS + 10-7 M testosterone (T), 10% NCS + 10-7 M testosterone + 10-6 M letrozole (T + L), 10% NCS + 10-7 M testosterone + 10-7 M exemestane (T+E). LetR-1 and ExeR-1 cells were withdrawn from testosterone and their respective AI one week before onset of experiment. β-actin was used as loading control. (C) CYP19A1 mRNA level in MCF-7 cells grown with 10% NCS + 10-7 M testosterone for five days and AI-resistant cell lines grown in their standard medium determined by quantitative RT-PCR

    Int J Oncol, 2015, 46(4):1481-90.. Exemestane purchased from Selleck.

Purity & Quality Control

Choose Selective Aromatase Inhibitors

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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF7a cells NELLS4hEgXSxdH;4bYNqfHliYYPzZZk> MX2xNEBl[Xm| M{fzNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjejIHPlcIx{KGW6cILld5NqdmdiVHX0MY9n\i1|YnX0ZWhUTDFvQYLvcUBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHRUXC2|dHnteYxifGWmIHPlcIwheHKxbHnm[ZJifGmxbjDt[YF{fXKnZDDh[pRmeiBzMDDkZZl{NCCHQ{WwQVUvPiCwTR?= MUGyNlk2OTB5NB?=
human MCF7 cells M2XDemN6fG:2b4jpZ4l1gSCjc4PhfS=> MWexNEB1dyBzNTFOwG0> MYCzMVYh\GG7cx?= MWXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDwcIFk\W62YXygcYlkem:|b33lJIFzd22jdHHz[UBmgHC{ZYPzbY5oKGi3bXHuJG1ETjdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHH0JFExKHSxIEG1JJVOKGGodHXyJFMhfG9iNjDkZZl{KGK7IF3UWEBie3OjeTDpckBxemW|ZX7j[UBw\iCnc4TyZYRqd2x? NU\afpRHOjV{N{ewOlY>

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:[1]
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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:[2]
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  • 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
    (Only for Reference)
Animal Research:[4]
+ Expand
  • Animal Models: estrogen-deficient ovariectomized (OVX) rats
  • Formulation: saline
  • Dosages: 100 mg/kg
  • Administration: Intramuscular injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 54 mg/mL (182.18 mM)
Ethanol 15 mg/mL (50.6 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 296.4
Formula

C20H24O2

CAS No. 107868-30-4
Storage powder
Synonyms FCE24304, PNU155971

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03024580 Not yet recruiting Breast Neoplasm Instituto Nacional de Cancer, Brazil|Cancer Research UK Cambridge Institute March 2017 Phase 2
NCT02947685 Not yet recruiting HER-2 Positive Breast Cancer|Estrogen Receptor Positive Breast Cancer Alliance Foundation Trials, LLC.|Pfizer|German Breast Group (GBG)|Fondazione Michelangelo|PrECOG, LLC.|The Australia and New Zealand Breast Cancer Trials Group (ANZBCTG)|Alliance Foundation Trials Biorepository - Washington State University|Alliance Foundation Trials Central Imaging Core Lab - Ohio State University|Mastering Breast Cancer Initiative, LLC|Mayo Clinic Statistics and Data Center|INC Research|SOLTI Breast Cancer Research Group February 2017 Phase 3
NCT02983604 Recruiting Advanced Estrogen Receptor Positive HER2- Breast Cancer Gilead Sciences January 2017 Phase 1|Phase 2
NCT02990845 Not yet recruiting Premenopausal Breast Cancer National Taiwan University Hospital|Merck Sharp & Dohme Corp. December 2016 Phase 1|Phase 2
NCT02598557 Recruiting Estrogen Receptor Positive|Postmenopausal|Stage 0 Breast Cancer|Stage I Breast Cancer|Stage IA Breast Cancer|Stage IB Breast Cancer|Stage II Breast Cancer|Stage IIA Breast Cancer|Stage IIB Breast Cancer National Cancer Institute (NCI) December 2016 Phase 2
NCT02917005 Not yet recruiting Metastatic Breast Cancer Hamdy A. Azim|Africa Middle East Cancer Intergroup November 2016 Phase 2

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Aromatase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID