Exemestane

Catalog No.S1196 Batch:S1196

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Technical Data

Formula

C20H24O2
Molecular Weight 296.4 CAS No. 107868-30-4
Solubility (25°C)* In vitro DMSO 54 mg/mL (182.18 mM)
Water Insoluble
Ethanol '15 mg/mL
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Exemestane is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
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. 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]
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]
Features 17-hydroexemestane is the principal metabolite of Exemestane.

Protocol (from reference)

Kinase Assay:

[1]
  • 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 this compound are incubated with 20 μg of microsomal protein, in the presence of a fixed amount (50 nM) of [3H]A.
Cell Assay:

[2]
  • 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
Animal Study:

[4]
  • Animal Models

    estrogen-deficient ovariectomized (OVX) rats

  • Dosages

    100 mg/kg

  • Administration

    Intramuscular injection

References

  • https://pubmed.ncbi.nlm.nih.gov/8043491/
  • https://pubmed.ncbi.nlm.nih.gov/17254854/
  • https://pubmed.ncbi.nlm.nih.gov/17079446/
  • https://pubmed.ncbi.nlm.nih.gov/15355898/
  • https://pubmed.ncbi.nlm.nih.gov/8476783/

Customer Product Validation

<p>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<sup>-7</sup> M testosterone (MCF-7) and LetR-1, LetR-3, ExeR-1 and ExeR-3 grown in their standard growth medium with 10<sup>-6</sup> M letrozole and 10<sup>-7</sup> 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<sup>-12</sup> M estradiol (E2), 10% NCS + 10<sup>-7 </sup>M testosterone (T), 10% NCS + 10<sup>-7</sup> M testosterone + 10<sup>-6</sup> M letrozole (T + L), 10% NCS + 10<sup>-7</sup> M testosterone + 10<sup>-7</sup> 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<sup>-7</sup> M testosterone for five days and AI-resistant cell lines grown in their standard medium determined by quantitative RT-PCR</p>

, , Int J Oncol, 2015, 46(4):1481-90.

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).

Data from [ , , Cell Physiol Biochem, 2017, 42(1):1-12 ]

Selleck's Exemestane Has Been Cited by 25 Publications

SERPINA3-ANKRD11-HDAC3 pathway induced aromatase inhibitor resistance in breast cancer can be reversed by HDAC3 inhibition [ Commun Biol, 2023, 6(1):695] PubMed: 37414914
SERPINA3-ANKRD11-HDAC3 pathway induced aromatase inhibitor resistance in breast cancer can be reversed by HDAC3 inhibition [ Commun Biol, 2023, 6(1):695] PubMed: 37414914
SERPINA3-ANKRD11-HDAC3 pathway induced aromatase inhibitor resistance in breast cancer can be reversed by HDAC3 inhibition [ Commun Biol, 2023, 6(1):695] PubMed: 37414914
Predicting clinical response to everolimus in ER+ breast cancers using machine-learning [ Front Mol Biosci, 2022, 9:981962] PubMed: 36304922
Predicting clinical response to everolimus in ER+ breast cancers using machine-learning [ Front Mol Biosci, 2022, 9:981962] PubMed: 36304922
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] PubMed: 35207746
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] PubMed: 35118583
Characterization of the Major Single Nucleotide Polymorphic Variants of Aldo-Keto Reductase 1C3 (Type 5 17β-Hydroxysteroid Dehydrogenase) [ J Steroid Biochem Mol Biol, 2022, S0960-0760(22)00072-3] PubMed: 35489629
Systems Pharmacology-Based Precision Therapy and Drug Combination Discovery for Breast Cancer [ Cancers (Basel), 2021, 13(14)3586] PubMed: 34298802
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4] PubMed: 34731453

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