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经验公式(希尔记法):
C20H24O2
化学文摘社编号:
分子量:
296.40
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
51111800
MDL number:
产品名称
依西美坦, ≥98% (HPLC)
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.
signalword
Danger
hcodes
Hazard Classifications
Aquatic Chronic 2 - Repr. 1B
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
涉药品监管产品
此项目有
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
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
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
Jürg Bernhard et al.
The Lancet. Oncology, 16(7), 848-858 (2015-06-21)
The combined efficacy analysis of the TEXT and SOFT trials showed a significant disease-free survival benefit with exemestane plus ovarian function suppression (OFS) compared with tamoxifen plus OFS. We present patient-reported outcomes from these trials. Between Nov 7, 2003, and
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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