|S1235||Letrozole||<1 mg/mL||57 mg/mL||<1 mg/mL|
|S1188||Anastrozole||<1 mg/mL||59 mg/mL||59 mg/mL|
|S1196||Exemestane||<1 mg/mL||54 mg/mL||15 mg/mL|
|S2208||Formestane||<1 mg/mL||61 mg/mL||<1 mg/mL|
|S1672||Aminoglutethimide||<1 mg/mL||20 mg/mL||7 mg/mL|
|S3784||Obacunone||-1 mg/mL||90 mg/mL||-1 mg/mL|
Letrozole is a third generation inhibitor of aromatase with IC50 of 0.07-20 nM in cell-free assays.It has no effect on the plasma levels of 17α-OH progesterone, thyroid-stimulating hormone (TSH), luteinizing hormone (LH), follicle-stimulating hormone (FSH), or androstenedione and does not affect normal urine electrolyte excretion or thyroid function in clinical studies.
Effect of aromatase inhibitor letrozole on cellular proliferation marker Ki-67 expression in LNCaP tumor xenografts. A, Ki-67 immunostaining in transverse sections of xenograft tumors from C, C＋T, C＋T＋D, C＋T＋L, and C＋T＋D＋L mice 2 days after testosterone replacement. Panel B, Quantification of Ki-67–positive cells in LNCaP tumors at day 2 post testosterone replacement. Error bars represent SEM. Number of animals in each group is shown in parentheses. ***, P ＜.0001.
Anastrozole is a third-generation nonsteroidal selective aromatase inhibitor. It may offer greater selectivity compared with other aromatase inhibitors, being without any intrinsic endocrine effects and with no apparent effect on the synthesis of adrenal steroids.
Cell viability analysis of BCSCs transduced as in A and treated with Anastrozole or Docetaxel, alone or in combination with BKM120 up to 72 hours. Data are mean ± SD of 3 independent experiments.
Exemestane is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
Effect of exemestane on phosphatidylserine exposure. A. Original histogram of annexin-V-binding of erythrocytes following exposure for 48 hours to Ringer solution without (grey area) and with (black line) presence of 40 µg/ml exemestane. B. Arithmetic means ± SEM (n = 24) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) exemestane (10-40 µg/ml). For comparison, the effect of the solvent DMSO is shown (grey bar). **(p<0.01),***(p<0.001) indicates significant difference from the absence of exemestane (ANOVA).
Formestane is a second generation selective aromatase inhibitor with an IC50 of 80 nM.
Aminoglutethimide is an aromatase inhibitor with IC50 of 10 μM.
Obacunone, a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. It significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; also a novel activator of Nrf2.