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Exemestane

Exemestane is a third generation aromatase inhibitor that prevents estrogen synthesis and is clinically used to treat ER+ breast cancer. Exemestane exhibits anticancer chemotherapeutic activity, inhibiting proliferation and inducing cell cycle arrest, apoptosis, and autophagy in breast cancer cells.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18922787

Cas No.

107868-30-4

Purity

≥98%

Formula

C20H24O2

Formula Wt.

296.40

Chemical Name

6-Methyleneandrosta-1,4-diene-3,17-dione

IUPAC Name

(8R,9S,10R,13S,14S)-10,13-dimethyl-6-methylidene-7,8,9,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-3,17-dione

Synonym

Aromasin; FCE-24304

Melting Point

188-191°C

Solubility

Soluble in methanol, ethanol (15 mg/mL), DMSO (54mg/mL) or dimethylformamide. Insoluble in water.

Appearance

Yellowish to off white powder

Amaral C, Borges M, Melo S, et al. Apoptosis and autophagy in breast cancer cells following exemestane treatment. PLoS One. 2012;7(8):e42398. PMID: 22912703.

Hong Y, Rashid R, Chen S. Binding features of steroidal and nonsteroidal inhibitors. Steroids. 2011 Jul;76(8):802-6. PMID: 21420422.

Bertelli G, Hall E, Ireland E, et al. Long-term endometrial effects in postmenopausal women with early breast cancer participating in the Intergroup Exemestane Study (IES)–a randomised controlled trial of exemestane versus continued tamoxifen after 2-3 years tamoxifen. Ann Oncol. 2010 Mar;21(3):498-505. PMID: 19717534.

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