Product Details
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112809-51-5 Name |
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Name |
Letrozole |
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Synonym |
LetrozoleUsp28;Letrozole99%;CGS-20267, Femara;LETRAZOLE;letrozolex;Lelrozol;1-[BIS(4-CYANOPHENYL)METHYL]-1,2,4-TRIAZOLE;4,4'-(1H-1,2,4-Triazol-1-ylmethylene)dibenzonitrile |
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112809-51-5 Biological Activity |
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Description |
Letrozole is an aromatase inhibitor with an IC50 of 1-13 nM. |
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Related Catalog |
Signaling Pathways >> Others >> Aromatase Signaling Pathways >> Autophagy >> Autophagy Research Areas >> Cancer |
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References |
[1]. Haynes, B.P., et al., The pharmacology of letrozole. J Steroid Biochem Mol Biol, 2003. 87(1): p. 35-45. [2]. Bhatnagar, A.S., et al., Highly selective inhibition of estrogen biosynthesis by CGS 20267, a new non-steroidal aromatase inhibitor. J Steroid Biochem Mol Biol, 1990. 37(6): p. 1021-7. [3]. Dellapasqua, S. and M. Colleoni, Letrozole. Expert Opin Drug Metab Toxicol, 2010. 6(2): p. 251-9. [4]. Lee, K., et al., An in vivo model of intratumoural aromatase using aromatase-transfected MCF7 human breast cancer cells. Int J Cancer, 1995. 62(3): p. 297-302. |
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112809-51-5 Chemical & Physical Properties |
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Melting point |
181-183ºC |
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Boiling point |
472.0±55.0 °C at 760 mmHg |
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Density |
1.1±0.1 g/cm3 |
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Molecular Formula |
C17H11N5 |
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Molecular Weight |
263.337 |
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Flash Point |
214.2±24.5 °C |
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PSA |
78.29000 |
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LogP |
3.70 |
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Exact Mass |
263.142242 |
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Vapour Pressure |
0.0±1.2 mmHg at 25°C |
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Index of Refraction |
1.615 |
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Storage condition |
-20°C Freezer |
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112809-51-5 Description |
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Letrozole is a potent, cell-permeable inhibitor of aromatase (IC50 = 2 nM). It inhibits proliferation of estrogen receptor-positive (ER+) MCF-7 cells when used alone at concentrations ranging from 0.1 to 100 nM and when used at a concentration of 10 nM in combination with testosterone or 4-androstene-3,17-dione. It also reduces matrix metalloproteinase-2 (MMP-2) and MMP-9 levels in MCF-7 cells when used at a concentration of 10 nM. Letrozole (10 μg per day) reduces tumor growth in an MCF-7Ca ovariectomized-mouse xenograft model. Formulations containing letrozole have been used in the treatment of postmenopausal breast cancer. |
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112809-51-5 Uses |
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Letrozole has been used: in organoid growth assay to determine its inhibitory capacity(48) to investigate steroid receptor coactivator-1 (SRC-1) mediated endogenous estrogen regulation of hippocampal PSD-95(49) to determine its effects on tumor-induced hyperalgesia(50) for hormonal manipulation in rats(51) to study its effects on lipocalin-2 (Lcn2)(52) to determine its effects on mechanical hyperalgesia and aromatase expression(53) |
