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Anastrozole

Anastrozole is a third generation aromatase inhibitor that suppresses synthesis of estrogen. Anastrozole exhibits anticancer chemotherapeutic activity and is clinically used to treat ER-positive breast cancer. In vitro, anastrozole inhibits proliferation of cancer cells by disrupting the mitochondrial membrane potential and inducing apoptosis. Because of its anti-estrogen properties, anastrozole may decrease bone mineral density and increase fracture risk.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18838647

Cas No.

120511-73-1

Purity

≥99%

Formula

C17H19N5

Formula Wt.

293.37

Chemical Name

2,2-(5-(IH-1,2,4-triazol-1-ylmethyl)-1,3-phenylene)bis(2-methylpropiononitrile)

IUPAC Name

2-[3-(2-cyanopropan-2-yl)-5-(1,2,4-triazol-1-ylmethyl)phenyl]-2-methylpropanenitrile

Synonym

ZD1033 Pure, Zeneca ZD1033

Melting Point

81-84°C

Solubility

soluble in methanol, acetone, ethanol (59 mg/mL), THF, ethyl acetate, chloroform, DMSO (40 mg/mL). Slightly soluble in water.

Appearance

White Crystal Powder

Kelly CM, Buzdar AU. Anastrozole. Expert Opin Drug Saf. 2010 Nov;9(6):995-1003. PMID: 20923259.

Hong Y, Chen S. Aromatase inhibitors: structural features and biochemical characterization. Ann N Y Acad Sci. 2006 Nov;1089:237-51. PMID: 17261771.

McCloskey E. Effects of third-generation aromatase inhibitors on bone. Eur J Cancer. 2006 May;42(8):1044-51. PMID: 16554149.

Xanthopoulos JM, Romano AE, Majumdar SK. Response of Mouse Breast Cancer Cells to Anastrozole, Tamoxifen, and the Combination. J Biomed Biotechnol. 2005;2005(1):10-19. PMID: 15689634.

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