exemestane

Exemestane (EXE) 是一种选择性的、具有口服活性的、不可逆的甾体芳香酶抑制剂，能够作用于人胎盘芳香酶 (IC50:30 nM) 和大鼠卵巢芳香酶 (IC50:40 nM)，可用于研究激素依赖性乳腺癌。

17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1,500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7aro cells in a concentration-dependent manner. 17β-hydroxy Exemestane (20 mg/kg) inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae, in ovariectomized rats.

Exemestane-d3 是 Exemestane 的氘代化合物。Exemestane 的 CAS 号为 107868-30-4。Exemestane 是一种选择性的、具有口服活性的、不可逆的甾体芳香酶抑制剂，能够作用于人胎盘芳香酶 (IC50:30 nM) 和大鼠卵巢芳香酶 (IC50:40 nM)，可用于研究激素依赖性乳腺癌。

Exemestane-13C-d3 是 Exemestane 的 13C 和氘代化合物。Exemestane 的 CAS 号为 107868-30-4。Exemestane 是一种选择性的、具有口服活性的、不可逆的甾体芳香酶抑制剂，能够作用于人胎盘芳香酶 (IC50:30 nM) 和大鼠卵巢芳香酶 (IC50:40 nM)，可用于研究激素依赖性乳腺癌。