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.
IC50&Target
IC50: 11.5 nM (aromatase)
体外研究
Letrozole (0.1-100 nM; 24-96 h) significantly inhibits growth of the MCF-7 epithelial breast cancer cells in a dose- and time-dependent manner.
Letrozole (10 nM) significantly suppresses the stimulatory effects of 4-androstene-3,17-dione or testosterone on MCF-7 cell proliferation.
Letrozole (10 nM; 24-48 h) suppresses the levels of secreted metalloproteinases (MMP‐2 and MMP‐9) in MCF-7 cells.
Cell Viability Assay
Cell Line:
MCF-7 cells
Concentration:
0.1, 1, 10, 100 nM
Incubation Time:
24, 48, 96 hours
Result:
Inhibited cells growth in a dose- and time-dependent manner.
体内研究
Letrozole (3-300 μg/kg; oral gavage once daily for 6 weeks) exhibits anti-tumor effects in rats.
Animal Model:
Adult female rats bearing mammary tumors
Dosage:
3, 10, 30, 100, 300 μg/kg
Administration:
Oral gavage once daily for 6 weeks
Result:
Induced complete regression of mammary tumors, with an ED50 of 10-30 μg/kg/day.
分子式
C17H11N5
分子量
285.30
CAS号
112809-51-5
中文名称
来曲唑
运输条件
Room temperature in continental US; may vary elsewhere.