Letrozole

Names

[ Name ]:
Letrozole

[Synonym ]:
4,4'-(1H-1,2,4-triazol-1-ylmethylene)bis(benzonitrile)
UNII-7LKK855W8I
Letrozol
Letoval
5-[Bis(4-methylphenyl)methyl]-1H-1,2,4-triazole
1H-1,2,4-Triazole, 5-[bis(4-methylphenyl)methyl]-
4,4'-(1H-1,2,4-Triazol-1-ylmethylene)bisbenzonitrile
Femera
MFCD00866241
[14C]-Letrozole
4,4'-((1H-1,2,4-Triazol-1-yl)methylene)dibenzonitrile
4-[(4-cyanophenyl)-(1,2,4-triazol-1-yl)methyl]benzonitrile
Femara
Letrozole

Biological Activity

[Description]:

Letrozole is an aromatase inhibitor with an IC50 of 1-13 nM.

[Related Catalog]:

Signaling Pathways >> Others >> Aromatase

Signaling Pathways >> Autophagy >> Autophagy

Research Areas >> Cancer

[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.

[Related Small Molecules]

Fadrozole | Exemestane | Endoxifen

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
472.0±55.0 °C at 760 mmHg

[ Melting Point ]:
181-183ºC

[ Molecular Formula ]:
C₁₇H₁₁N₅

[ Molecular Weight ]:
263.337

[ Flash Point ]:
214.2±24.5 °C

[ Exact Mass ]:
263.142242

[ PSA ]:
78.29000

[ LogP ]:
3.70

[ Vapour Pressure ]:
0.0±1.2 mmHg at 25°C

[ Index of Refraction ]:
1.615

[ Storage condition ]:
-20°C Freezer

MSDS

Click to get detail MSDS

Safety Information

[ Hazard Codes ]:
Xi: Irritant;C: Corrosive;

[ Risk Phrases ]:
R36/37/38

[ Safety Phrases ]:
26-36

[ RIDADR ]:
NONH for all modes of transport

[ RTECS ]:
DI4957000

[ HS Code ]:
2933990090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

Comparison of tamoxifen and letrozole response in mammary preneoplasia of ER and aromatase overexpressing mice defines an immune-associated gene signature linked to tamoxifen resistance.

Carcinogenesis 36(1) , 122-32, (2015)

Response to breast cancer chemoprevention can depend upon host genetic makeup and initiating events leading up to preneoplasia. Increased expression of aromatase and estrogen receptor (ER) is found in...

Hypogonadism Associated with Cyp19a1 (Aromatase) Posttranscriptional Upregulation in Celf1 Knockout Mice.

Mol. Cell. Biol. 35 , 3244-53, (2015)

CELF1 is a multifunctional RNA-binding protein that controls several aspects of RNA fate. The targeted disruption of the Celf1 gene in mice causes male infertility due to impaired spermiogenesis, the ...

Aromatase (Cyp19a1b) in the pituitary is dynamically involved in the upregulation of lhb but not fshb in the vitellogenic female ricefield eel Monopterus albus.

Endocrinology 155(11) , 4531-41, (2014)

Aromatase, encoded by Cyp19a1, is expressed in the pituitary of vertebrates; however, its physiological relevance remains poorly defined. In teleosts, the duplicated cyp19a1b is preferentially express...