Formestane
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- CAS-Nr.
- 566-48-3
- Englisch Name:
- Formestane
- Synonyma:
- 4-OHA;CYPXIX;LENTARON;CGP-32349;P-450AROM;FORMESTANE;FROMESTANE;NSC 282175;Stan FuMei;FORMESTAQNE
- CBNumber:
- CB6251183
- Summenformel:
- C19H26O3
- Molgewicht:
- 302.41
- MOL-Datei:
- 566-48-3.mol
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Formestane Eigenschaften
- Schmelzpunkt:
- 199-202°C
- alpha
- D20 +181° (c = 7.7 in chloroform)
- Siedepunkt:
- 383.44°C (rough estimate)
- Dichte
- 1.1189 (rough estimate)
- Brechungsindex
- 1.4200 (estimate)
- storage temp.
- 2-8°C
- Löslichkeit
- Chloroform (Slightly), Methanol (Slightly)
- Aggregatzustand
- solid
- pka
- 9.31±0.60(Predicted)
- Farbe
- White to Off-White
- InChI
- InChI=1S/C19H26O3/c1-18-10-8-15(20)17(22)14(18)4-3-11-12-5-6-16(21)19(12,2)9-7-13(11)18/h11-13,22H,3-10H2,1-2H3/t11-,12-,13-,18+,19-/m0/s1
- InChIKey
- OSVMTWJCGUFAOD-KZQROQTASA-N
- SMILES
- C1(=O)C(O)=C2[C@](C)(CC1)[C@]1([H])[C@]([H])([C@@]3([H])[C@@](CC1)(C)C(=O)CC3)CC2
- CAS Datenbank
- 566-48-3(CAS DataBase Reference)
Sicherheit
- Risiko- und Sicherheitserklärung
- Gefahreninformationscode (GHS)
Kennzeichnung gefährlicher |
T |
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R-Sätze: |
60 |
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S-Sätze: |
53-36/37/39-45 |
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WGK Germany |
3 |
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RTECS-Nr. |
BV8152500 |
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Bildanzeige (GHS) |
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Alarmwort |
Achtung |
Gefahrenhinweise |
Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
H360 |
Kann die Fruchtbarkeit beeinträchtigen oder das Kind im Mutterleib schädigen. |
Fertility (Fruchtbarkeit) |
Kategorie 1 |
Achtung |
src="/GHS08.jpg" width="20" height="20" /> |
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Sicherheit |
P201 |
Vor Gebrauch besondere Anweisungen einholen. |
P308+P313 |
BEI Exposition oder falls betroffen: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen. |
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Formestane Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R60:Kann die Fortpflanzungsfähigkeit beeinträchtigen.
S-Sätze Betriebsanweisung:
S53:Exposition vermeiden - vor Gebrauch besondere Anweisungen einholen.
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Beschreibung
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.
Chemische Eigenschaften
Needles
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.
Mechanism of action
Aromatase inhibitors such as formestane and letrozole reduce plasma estradiol levels by inhibiting the conversion of testosterone to estrogen. This compound was first described as a competitive inhibitor, but subsequent evidence proved that its binding to aromatase was irreversible. Hence, it is a suicide inhibitor. In the dog, but not rodents, this results in Leydig cell hypertrophy and hyperplasia. This is thought to be due to the differential sensitivity of the pituitary feedback mechanism to estrogens and androgens in the different species[1-2].
Formestane Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Osmiumtetraoxid
Kaliumhydroxid
Natriumsulfat
2-Methylpropanol-2
Acetylacetone
Sodium bisulfite solution
Ethylacetat
Dichlormethan
Natriumcarbonat
Androst-4-ene-3,17-dione, 2-hydroxy-, (2α)-
Androstan-17-one, 3,4-dihydroxy-, (3α,4β,5α)-
Androstane-3,17-dione, 4,5-dihydroxy- (6CI,9CI)
4-ANDROSTEN-4-OL-3,17-DIONE 4-METHYLETHE R
Androst-3-en-17-one,(5)
Androst-4-en-3,17-dion
Downstream Produkte
Formestane Anbieter Lieferant Produzent Hersteller Vertrieb Händler.
Global( 253)Lieferanten
566-48-3()Verwandte Suche:
- 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
- FROMESTANE
- FORMESTANE
- FORMESTAQNE
- LENTARON
- Formesatane
- FORMESTANE 98%
- FORMESTANE,4-HYDROXYANDROST-4-ENE-3,17-DIONE
- 4-ANDROSTENE-4-OL-3,17-DIONE
- 4-Hydroxyandrost-4-ene-3,17-dione, 4-OHA, CGP-32349, Lentaron
- FORMASTANE/FORMESTANE/4-ANDROSTEN-4-OL-3,17-DIONE
- 4-ANDROSTEN-4-OL-3,17-DIONE(FORMESTANE)
- B, Aromatase inhibitor
- 6-hydroxy-10,13-dimethyl-
1,7,8,9,10,11,12,13,15,16-decahydro-2H-cyclopenta[a]phenanthrene-3,17(6H,14H)-dione
- 4-Hydroxyandrost-4-ene-3,17-dione, CGP-32349
- 4-Hydroxyandrostan-4-ene-3,17-dione
- (8R,9S,10R,13S,14S)-4-hydroxy-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthrene-3,17-dione
- (8R,9S,10R,13S,14S)-4-hydroxy-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthrene-3,17-quinone
- 4-Hydroxy-4-androstenedione
- 4-Hydroxyandrostendione (Formestane)
- NSC 282175
- CGP-32349:Lentaron
- Androst-4-ene-3,17-dione,4-hydroxy-
- Stan FuMei
- (8R,9S,10R,13S,14S)-4-hydroxy-10,13-dimethyl-1,7,8,9,10,11,12,13,15,16-decahydro-2H-cyclopenta[a]phenanthrene-3,17(6H,14H)-dione
- Anti-Cytochrome P450 19A1 antibody produced in rabbit
- CYPXIX
- Cytochrome P450 19A1
- Estrogen synthetase
- P-450AROM
- Lentaron Formestane
- Formestane on sale CAS NO.566-48-3
- Formestane ,Lentaron
- Formestane cas 566-48-3 (skype:lisa_21819)
- Formestane 566-48-3
- Formestane USP/EP/BP
- Anti-Estrogens Steroids Raw Powder Formestane
- Formestane(4-hydroxy-androstenedione)
- Formestane (CGP-32349)
- TIANFU CHEM- Formestane
- Formestane Lentaron Raw Powder
- 566-48-3
- Enzymes, Inhibitors, and Substrates
- Enzyme Inhibitors
- Enzyme Inhibitors by Enzyme
- 多肽抗原
- 小鼠抗人和大、小鼠、犬、猪、牛芳香化酶多克隆抗体
- Aromatase
- A to C
- Biochemicals and Reagents
- BioChemical