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Merck
CN

182541

Aromatase Inhibitor II, Letrozole

The Aromatase Inhibitor II, Letrozole, also referenced under CAS 112809-51-5, controls the biological activity of Aromatase.

Synonym(s):

Aromatase Inhibitor II, Letrozole, 4,4ʹ-(1H-1,2,4-Triazol-1-ylmethylene)dibenzonitrile, 1-( bis-(4-Cyanophenyl)methyl)-1,2,4-triazole

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About This Item

Empirical Formula (Hill Notation):
C17H11N5
CAS Number:
112809-51-5
Molecular Weight:
285.30
UNSPSC Code:
12352200
MDL number:
MFCD00866241

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InChI

1S/C17H11N5/c18-9-13-1-5-15(6-2-13)17(22-12-20-11-21-22)16-7-3-14(10-19)4-8-16/h1-8,11-12,17H

InChI key

HPJKCIUCZWXJDR-UHFFFAOYSA-N

assay

≥99% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

ethanol: <5 mg/mL (partially soluble), DMSO: 50 mg/mL, clear, colorless

shipped in

ambient

Quality Level

100

General description

An orally bioavailable non-steroidal triazole compound that acts as a potent and selective inhibitor of aromatase (IC50 = 140, 350 and 450 pM in Dex-treated fibroblasts, MCF-7Ca, and JEG-3 cells, respectively). Competitively, but reversibly binds to the heme iron of aromatase. Does not affect the synthesis of adrenal mineralocorticoid or glucocorticoids. Reported to be highly effective as an anti-estrogenic and anti-proliferative agent in estrogen-rich tumors. Also delays the fusing of the growth plates in adolescents and enhances the effectiveness of growth hormone. Shown to synergistically induce apoptosis and cause tumor regression when combined with IGF-1R inhibitors.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Hou, X., et al. 2011. Cancer Res.71, 7597.
Lisztwan, J., et al. 2008. Breast Cancer Res.10, R56.
Miller, W.R., et al. 2002. Cancer Invest.20 (Suppl 2), 15.
Long, B.J., et al. 1998. J. Steroid Biochem. Molec. Biol.67, 293.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

pictograms

Health hazard
GHS08

signalword

Warning

Hazard Classifications

Repr. 2 - STOT RE 2

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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