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Formestane

Anti-cancer drugs Chemical Properties Uses production method
Formestane
Formestane structure
CAS No.
566-48-3
Chemical Name:
Formestane
Synonyms
4-OHA;CYPXIX;LENTARON;CGP-32349;P-450AROM;FORMESTANE;FROMESTANE;NSC 282175;Stan FuMei;FORMESTAQNE
CBNumber:
CB6251183
Molecular Formula:
C19H26O3
Formula Weight:
302.41
MOL File:
566-48-3.mol

Formestane Properties

Melting point:
199-202°C
alpha 
D20 +181° (c = 7.7 in chloroform)
Boiling point:
383.44°C (rough estimate)
Density 
1.1189 (rough estimate)
refractive index 
1.4200 (estimate)
storage temp. 
2-8°C
form 
solid
InChIKey
OSVMTWJCGUFAOD-KZQROQTASA-N
CAS DataBase Reference
566-48-3(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  T
Risk Statements  60
Safety Statements  53-36/37/39-45
WGK Germany  3
RTECS  BV8152500
Symbol(GHS):
Signal word: Danger
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H360 May damage fertility or the unborn child Reproductive toxicity Category 1A, 1B Danger
Precautionary statements:
P201 Obtain special instructions before use.
P308+P313 IF exposed or concerned: Get medical advice/attention.

Formestane price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich F2552 Formestane solid 566-48-3 1g $174 2018-11-20 Buy
Cayman Chemical 18282 4-hydroxy Androstenedione ≥98% 566-48-3 1g $150 2018-11-13 Buy
Cayman Chemical 18282 4-hydroxy Androstenedione ≥98% 566-48-3 100mg $25 2018-11-13 Buy
Cayman Chemical 18282 4-hydroxy Androstenedione ≥98% 566-48-3 500mg $94 2018-11-13 Buy

Formestane Chemical Properties,Uses,Production

Anti-cancer drugs

Formestane 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 Properties

Crystallized 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).

Uses

aromatase inhibitors ,it is used for progressive breast cancer.
male hormones, assimilating protein class.

production method

Androst-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).

Description

Formestane is a potent aromatase inhibitor launched in the UK as a second-line endocrine treatment for breast cancer. As a synthetic derivative of androstanedione, the natural substrate for the biosynthesis of estrogen by the enzyme aromatase, formastane selectively inhibits aromatase and binds to its steroid receptor site to cause a rapid and sustained fall in circulating estrogen level and, therefore, inhibits tumor growth. In patients with existing bulky primary tumors, formestane effectively reduces the size of the tumors. Formastane has apparent tolerability advantages and less side effects than other agents such as aminoglutethimide.

Chemical Properties

Needles

Originator

Ciba-Geigy (Switzerland)

Uses

An antitumor drug. An aromatase inhibitor

Uses

antineoplastic, aromatase inhibitor

Definition

ChEBI: 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.

brand name

Lentaron

Formestane Preparation Products And Raw materials

Raw materials

Preparation Products


Formestane Suppliers

Global( 165)Suppliers
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Shenzhen Sendi Biotechnology Co.Ltd.
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Hebei Huanhao Biotechnology Co., Ltd.
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View Lastest Price from Formestane manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-12-21 Formestane
566-48-3
US $1.00 / kg 1kg 99% Customized career henan chemical co
2019-01-21 Formestane on sale CAS NO.566-48-3
566-48-3
US $100.00 / Kg 1Kg 99% 5000KG Hebei Chisure Biotechnology Co., Ltd.
2018-12-03 Formestane cas 566-48-3 (skype:lisa_21819)
566-48-3
US $60.00 / KG 1KG 99% 20tons Hebei Huanhao Biotechnology Co., Ltd.

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