Licensed by Pfizer Catalog No.S1196 Synonyms: FCE24304, PNU155971
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.
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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 LetR-1 and ExeR-1 cells were withdrawn from testosterone and their respective AI one week before onset of experiment.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
|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.|
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.  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.  Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells. 
|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.  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. |
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.
-  Di Salle E, et al. J Steroid Biochem Mol Biol, 1994, 49(4-6), 289-294.
-  Miki Y, et al. Bone, 2007, 40(4), 876-887.
-  Wang X, et al. Cancer Res, 2006, 66(21), 10281-10286.
|In vitro||DMSO||54 mg/mL (182.18 mM)|
|Ethanol||15 mg/mL (50.6 mM)|
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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|
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.
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