ExemestaneLicensed by Pfizer 107868-30-4

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Molecular Weight:

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

Biological Activity

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.


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.

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Product Categories : Endocrinology & Hormones > Aromatase Inhibitor