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Merck

PZ0006

Exemestane

≥98% (HPLC)

Sinónimos:

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

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Acerca de este artículo

Fórmula empírica (notación de Hill):
C20H24O2
Número CAS:
Peso molecular:
296.40
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
51111800
MDL number:
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InChI

1S/C20H24O2/c1-12-10-14-15-4-5-18(22)20(15,3)9-7-16(14)19(2)8-6-13(21)11-17(12)19/h6,8,11,14-16H,1,4-5,7,9-10H2,2-3H3/t14-,15-,16-,19+,20-/m0/s1

SMILES string

C[C@]12CC[C@H]3[C@@H](CC(=C)C4=CC(=O)C=C[C@]34C)[C@@H]1CCC2=O

InChI key

BFYIZQONLCFLEV-DAELLWKTSA-N

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D +250 to +300°, c = 1 in methanol

color

white to off-white

solubility

DMSO: ≥20 mg/mL

storage temp.

2-8°C

Quality Level

Gene Information

human ... CYP19A1(1588)

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Biochem/physiol Actions

Exemestane is a steroidal antiestrogen and irreversible aromatase inhibitor. Exemestane acts as a false substrate for the aromatase enzyme. Exemestane also prevents the conversion of androgens to estrogens and is used to treat estrogen-dependent breast cancer.
Exemestane is a steroidal antiestrogen; aromatase inhibitor.

Features and Benefits

This compound is featured on the Nuclear Receptors (Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

pictograms

Health hazardEnvironment

signalword

Danger

hcodes

Hazard Classifications

Aquatic Chronic 2 - Repr. 1B

Clase de almacenamiento

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

flash_point_f

Not applicable

flash_point_c

Not applicable


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Anneleen Lintermans et al.
Expert opinion on drug safety, 10(3), 473-487 (2011-03-25)
Hormone-dependent breast cancer can be successfully treated by either blocking the estrogen receptor, as with tamoxifen, or reducing the production of estrogens, as with aromatase inhibitors. Exemestane is a third-generation aromatase inhibitor used in the treatment of estrogen-receptor-positive breast cancer
Michael Gnant et al.
Journal of the National Cancer Institute, 105(9), 654-663 (2013-02-22)
Breast Cancer Trials of Oral Everolimus 2 (BOLERO-2), a phase III study in postmenopausal women with estrogen receptor-positive breast cancer progressing despite nonsteroidal aromatase inhibitor therapy, showed statistically significant benefits with adding everolimus to exemestane. Moreover, in preclinical studies, mammalian
Duveken B Y Fontein et al.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 31(18), 2257-2264 (2013-04-24)
Specific adverse events (AEs) associated with endocrine therapy and related to depletion or blocking of circulating estrogens may be related to treatment efficacy. We investigated the relationship between survival outcomes and specific AEs including vasomotor symptoms (VMSs), musculoskeletal adverse events
Nan Soon Wong et al.
Expert opinion on pharmacotherapy, 6(13), 2353-2363 (2005-10-13)
Breast cancer is a major health problem in developed countries. Endocrine therapy is a key component in the management of hormone receptor-positive disease. Although tamoxifen has historically been the gold standard in the first-line management of early and advanced breast
Willemien van de Water et al.
The oncologist, 18(1), 8-13 (2012-12-25)
For postmenopausal patients with hormone-sensitive breast cancer, outcome is worse with increasing age at diagnosis. The aim of this study was to assess the incidence of breast cancer recurrence (locoregional and distant), and contralateral breast cancer by age at diagnosis.

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