Exemestane

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 K_i of 4.3 nM. Exemestane displaces [³H]5α-dihydrotestosterone from rat prostate androgen receptor with IC₅₀ of 0.9 μM^[1].
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].