17beta-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17beta-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor alpha (ERalpha, IC50 = 21.2 µM). 17beta-Hydroxy exemestane stimulates growth of AR- and ERalpha-positive MCF-7 (EC50= 2.7 µM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17beta-Hydroxy exemestane 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[1][2][3][4][5].
Molecular Weight:
298.42
CAS Number:
[122370-91-6]
Formula:
C20H26O2
Target:
Androgen Receptor,Estrogen Receptor/ERR,LDLR
Application Notes:
MCE Product type: Reference compound
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