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Exemestane (Synonyms: FCE 24304; EXE)

Cat. No.: HY-13632 Purity: 99.95%
Handling Instructions

Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.

For research use only. We do not sell to patients.

Exemestane Chemical Structure

Exemestane Chemical Structure

CAS No. : 107868-30-4

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 115 In-stock
Estimated Time of Arrival: December 31
100 mg USD 144 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].

IC50 & Target

IC50: 30 nM (Human placenta aromatase) and 40 nM (Rat ovarian aromatase)[1]

In Vitro

Exemestane (EXE; 1-1000 nM; 72 hours; hFOB, Saos-2 cells<) treatment significantly increases the number of the cells[2].
Exemestane (0.1- μM; 72 hours) 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 competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. Exemestane displaces [3H]5α-dihydrotestosterone from rat prostate androgen receptor with IC50 of 0.9 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: hFOB, Saos-2 cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 72 hours
Result: Induced cell proliferation.
In Vivo

Exemestane (EXE; 20-100 mg/kg; intramuscular injection; once weekly; for 16 weeks) treatment significantly increases the lumbar vertebral and femoral BMD, bending strength of the femur, compressive strength of the fifth lumbar vertebra, and trabecular bone volume. Exemestane significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin. Exemestane causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol[3].
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[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Sprague Dawley rats (10-month-old) bearing ovariectomy [3]
Dosage: 20 mg/kg, 50 mg/kg, or 100 mg/kg
Administration: Intramuscular injection; once weekly; for 16 weeks
Result: Significantly increased the lumbar vertebral and femoral BMD, bending strength of the femur, compressive strength of the fifth lumbar vertebra, and trabecular bone volume.
Clinical Trial
Molecular Weight

296.40

Formula

C₂₀H₂₄O₂

CAS No.

107868-30-4

SMILES

C[[email protected]]1([[email protected]](CC2)([H])[[email protected]]3([H])CC(C4=CC(C=C[[email protected]]4(C)[[email protected]@]3([H])CC1)=O)=C)C2=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 54 mg/mL (182.19 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3738 mL 16.8691 mL 33.7382 mL
5 mM 0.6748 mL 3.3738 mL 6.7476 mL
10 mM 0.3374 mL 1.6869 mL 3.3738 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.43 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.43 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ExemestaneFCE 24304 EXEFCE24304FCE-24304AromataseSteroidalaromataseandrostenedionealkalinephosphatase5α-dihydrotestosteroneInhibitorinhibitorinhibit

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