Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity.
Fadrozole hydrochloride hemihydrate is an orally active, potent, selective and nonsteroidal aromatase inhibitor, with an IC50 of 6.4 nM. Fadrozole hydrochloride hemihydrate inhibits the production of estrogen and progesterone, with IC50 values of 0.03 and 120 μM. Fadrozole hydrochloride hemihydrate shows prevention of spontaneous tumours. Fadrozole hydrochloride hemihydrate can be used for the research of estrogen-dependent disease and cancer[1][2][3].
Eriodictyol chalcone possesses both anti-aromatase and an anti-17β-HSD activity[1].
Aromatase-IN-2 is a potent Aromatase inhibitor with an IC50 value of 1.5 µM[1].
Isolimonexic acid is a limonoid isolated from lemon (Citrus lemon L. Burm) seed, has anti-cancer and anti-aromatase (IC50=25.60 μM) properties[1].
7-Hydroxyflavanone is an aromatase (cytochrome P450 19; CYP19) inhibitor with an IC50 of 65 μM[1].
Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor with a Ki of 0.18 μM. Androsta-1,4,6-triene-3,17-dione inhibits estrogen biosynthesis and shows antifertility effects. Androsta-1,4,6-triene-3,17-dione induces impairment of spatial memory[1][2].
Vorozole is a potent and selective, orally active non-steroidal aromatase inhibitor[1][2]. Vorozole shows antitumor activity in vivo. Vorozole has the potential for the research of mammary cancer[3].
Letrozole is an aromatase inhibitor with an IC50 of 1-13 nM.
Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity[1]. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase[2].
Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
(R)-(+)-Aminoglutethimide is a potent and orally active aromatase inhibitor. (R)-(+)-Aminoglutethimide has the potential for the research of breast cancer[1].
Letrozole-d4 (CGS 20267-d4) is the deuterium labeled Letrozole. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer[1][2][3].
Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.Target: AromataseApproved: October 2005Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. Exemestane displaces [3H]DHT from rat prostate androgen receptor with IC50 of 0.9 μM [1]. Exemestane (1 μM) 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 causes aromatase degradation in a dose-responsive manner in MCF-7aro cells [3].Exemestane increases lumbar spine BMD by 14.0% in OVX rats at dose of 100 mg/kg. Exemestane (100 mg/kg) and 17-hydroexemestane (20 mg/kg) significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin in rats and causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol inOVX rats [4].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 [5].
Fadrozole is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively[1].
Org30958 is a potent aromatase inhibitor in vivo.
Fadrozole hydrochloride is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
SYN20028567 is an aromatase (CYP19) inhibitor with an IC50 of 9.4 nM. SYN20028567 can be used for breast cancer research[1].