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Formestane

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Products Intro: Product Name:Formestane
CAS:566-48-3
Purity:99% Package:10.8/G
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Products Intro:Product Name:ForMestane
CAS:566-48-3
Purity:99%
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Products Intro:Product Name:Formestane;4-hydroxy-androst-4-ene-17-dione;4-hydroxy-delta(sub4)-androstenedione;4-HYDROXYANDROST-4-ENE-3,17-DIONE;4-HYDROXYANDROSTENEDIONE;4-HYDROXY-4-ANDROSTENE-3,17-DIONE;4-ANDROSTEN-4-OL-3,17-DIONE;4-OHA;CGP-32349
CAS:566-48-3
Purity:99% Package:1kg,5kg;10kg,25kg
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Products Intro:Product Name:Formestane
CAS:566-48-3
Package:100MG
Company Name: Pure Chemistry Scientific Inc.  
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Products Intro:Product Name:ForMestane;4-Hydroxy-testosterone
CAS:566-48-3
Purity:98% Package:100Mg;1g
Formestane Basic information
Anti-cancer drugs Chemical Properties Uses production method
Product Name:Formestane
Synonyms:4-hydroxy-androst-4-ene-17-dione;4-hydroxy-delta(sub4)-androstenedione;4-HYDROXYANDROST-4-ENE-3,17-DIONE;4-HYDROXYANDROSTENEDIONE;4-HYDROXY-4-ANDROSTENE-3,17-DIONE;4-ANDROSTEN-4-OL-3,17-DIONE;4-OHA;CGP-32349
CAS:566-48-3
MF:C19H26O3
MW:302.41
EINECS:
Product Categories:Pharmaceutical Raw Materials;Miscellaneous Biochemicals;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Steroids;Anti-cancer&immunity
Mol File:566-48-3.mol
Formestane Structure
Formestane Chemical Properties
Melting point 199-202°C
alpha D20 +181° (c = 7.7 in chloroform)
storage temp. 2-8°C
form solid
InChIKeyOSVMTWJCGUFAOD-KZQROQTASA-N
CAS DataBase Reference566-48-3(CAS DataBase Reference)
Safety Information
Hazard Codes T
Risk Statements 60
Safety Statements 53-36/37/39-45
WGK Germany 3
RTECS BV8152500
MSDS Information
ProviderLanguage
Formestane English
SigmaAldrich English
Formestane Usage And Synthesis
Anti-cancer drugsFormestane also known as lentaron,is an anti-cancer drug, it is primarily used for the treatment of postmenopausal women with advanced breast cancer, it is also effective in prostate cancer.
Formestane is a androstenedione derivative, and it belongs to an aromatase inhibitor with aminoglutethimide, it is a hormone antineoplastic agent. In physiological conditions, it may competitively inhibit the synthesis of the enzyme leading to estrogen biosynthesis decrease in tissues, then it plays its role in cancer. When the tumor tissue growth relies on the presence of estrogen, in order to inhibit tumor growth, the elimination of tumor estrogen-mediated growth stimulation is necessary. This product is more selective than aminoglutethimide while its activity is 100 to 1000 times of aminoglutethimide, and it does not inhibit the synthesis of adrenal hormones,without having to recharge cortisone, etc . The in vitro inhibition of aromatase enzyme of this product is 60 times stronger than aminoglutethimide.
While it is used alone, the drug can not significantly reduce the pre-menopausal estrogen levels in the blood of women,when it is combined with goserelin (gonadotropin-releasing hormone agonist), its inhibitory effect of estrogen in premenopausal women is greater than goserelin used alone. Formestane has no cross-resistance with other aromatase inhibitors , it has no side effects of aminoglutethimide. After oral administration,it is rapidly absorbed by gastrointestinal, its peak plasma concentration time is 1 to 1.5 hours, but the peak concentration of individual is of great difference; after intramuscular injection,it can be accumulated at the injection site and be slowly absorbed. It performs Biphasic elimination process, the initial elimination half-life is 2 to 4 days, the terminal elimination half-life is 5 to 10 days. It is mainly metabolized in the liver after oral administration, in the form of glycosides acid metabolites excreted in the urine.
The above information is edited by the chemicalbook of Tian Ye.
Chemical PropertiesCrystallized from aqueous methanol, m.p. 199~202 ℃; crystallized from ethyl acetate, m.p. 203.5~206 ℃. UV absorption maximum (99.5% ethanol): 278nm (ε11030). [α] D20 + 181 ° (C = 7.7, chloroform).
Usesaromatase inhibitors ,it is used for progressive breast cancer.
male hormones, assimilating protein class.
production methodAndrost-4-ene-3,17-dione (Ⅰ) (1.432g, 5mmo1) is dissolved in 50ml tert-butanol ,add 38mg (0.15mmo1) osmium tetroxide in 2ml t-butanol solution at room temperature, and then 5ml 35% hydrogen peroxide is added, followed by stirring at room temperature for 3 days. After dilution of 100ml brine, and extract with dichloromethane (2 × 100m1). The extract is washed with 100ml brine, , 50ml 10% sodium bisulfite solution, 50ml 10% sodium carbonate solution and 100ml brine, dry over anhydrous sodium sulfate, and concentrate. The residue (1.824g) of the compound (Ⅱ), is dissolved in methanol (10ml),add potassium hydroxide (393mg, 7mmo1) in 3ml methanol . Plus Albert, stirring 10min at 55 ℃. Add 0.3ml of acetic acid and 100ml of brine, and extract with dichloromethane (2 × 100ml). Complex solution, combine, wash with 100ml brine, dry with anhydrous sodium sulfate, and concentrate. The residue (1.727g) by column chromatography on silica gel, wash with hexane-ethyl acetate (7: 3) to give 715mg formestane, yield 47%, mp 200~202 ℃ (acetone).
Chemical PropertiesNeedles
UsesAn antitumor drug. An aromatase inhibitor
Usesantineoplastic, aromatase inhibitor
DefinitionChEBI: A 17-oxo steroid that is androst-4-ene-3,17-dione in which the hydrogen at position 4 is replaced by a hydroxy group. Formestane was the first selective, type I steroidal aromatase inhibitor, suppressing oestrogen production from anabolic steroids or proho mones. It was formerly used in the treatment of oestrogen-receptor positive breast cancer in post-meopausal women. As it has poor oral bioavailability, it had to be administered by (fortnightly) intramuscular injection. It fell out of use with the subseque t development of cheaper, orally active aromatase inhibitors. Formestane is listed by the World Anti-Doping Agency as a substance prohibited from use by athletes.
Formestane Preparation Products And Raw materials
Raw materialsEthyl acetate-->Dichloromethane-->Sodium carbonate-->Sodium sulfate-->Potassium hydroxide -->tert-Butanol-->Acetylacetone-->Osmium tetraoxide
Tag:Formestane(566-48-3) Related Product Information
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