Letrozole is an orally-available, triazole-based inhibitor of the aromatase enzyme complex at an IC50 range of 1-13 nM. It is known to be a Cytochrome P450 inhibitor as well as an estrogen antagonist and has shown promise in the treatment of breast cancer in postmenopausal women. (1, 2)
Letrozole was also found to be a potent in vitro inhibitor of cell proliferation and of type IV collagenases expressed by ER-positive MCF-7 cells. Treatment of MCF-7 cells with 10 nM letrozole led to significant inhibition of MMP levels. Furthermore, concurrent treatment with 17-b-estradiol greatly suppressed estradiol-induced stimulation of MMP levels. (3)
Technical information:
Chemical Formula: | C17H11N5 | |
CAS #: | 112809-51-6 | |
Molecular Weight: | 285.3 | |
Purity: | > 98% | |
Appearance: | white | |
Chemical Name: | 4,4'-((1H-1,2,4-triazol-1-yl)methylene)dibenzonitrile | |
Solubility: | Up to 100 mM in DMSO | |
Synonyms: | 0 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
1. | Haynes et al., The pharmacology of letrozole. J. Steroid Biochem. Mol. Biol. 2003, 87, 35-45. Pubmed ID: 14630089 |
2. | Dellapasqua et al., Letrozole. Expert Opin. Drug Metab. Toxicol. 2010, 6(2), 251-259. Pubmed ID: 20095792 |
3. | Mitropoulou et al., LETROZOLE AS A POTENT INHIBITOR OF CELL PROLIFERATION AND EXPRESSION OF METALLOPROTEINASES (MMP-2 AND MMP-9) BY HUMAN EPITHELIAL BREAST CANCER CELLS. Int. J. Cancer, 2003, 104, 155-160. Pubmed ID: 12569569 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.