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Exemestane

CAS No. : 107868-30-4

MCE 站：Exemestane

产品活性：Exemestane (FCE 24304) 是一种选择性，不可逆和具有口服活性的甾体芳香酶 (aromatase) 抑制剂，对人胎盘和大鼠卵巢芳香酶的 IC₅₀ 分别为 30 nM 和 40 nM。Exemestane 可用于激素依赖性乳腺癌研究。

研究领域：Others

作用靶点：Aromatase

In Vitro: Exemestane (EXE; 1-1000 nM; 72 hours; hFOB, Saos-2 cells<) treatment significantly increases the number of the cells.
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.
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.

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.
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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