4-HYDROXYTAMOXIFEN

Bezeichnung:4-HYDROXYTAMOXIFEN

CAS-Nr68047-06-3

Englisch Name:4-HYDROXYTAMOXIFEN

CBNumberCB0754622

SummenformelC26H29NO2

Molgewicht387.51

MOL-Datei68047-06-3.mol

4-HYDROXYTAMOXIFEN physikalisch-chemischer Eigenschaften

Schmelzpunkt	105-107°C
Siedepunkt	513.45°C (rough estimate)
Dichte	1.1005 (rough estimate)
Brechungsindex	1.6000 (estimate)
storage temp.	2-8°C
Löslichkeit	95% ethanol: 20 mg/mL
pka	10.35±0.15(Predicted)
Aggregatzustand	powder
Farbe	white
Stabilität	Stable. Store cool. Incompatible with strong oxidizing agents.
InChIKey	TXUZVZSFRXZGTL-OCEACIFDSA-N
CAS Datenbank	68047-06-3

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	20/21/22-63
S-Sätze:	22-23-36
WGK Germany	3
RTECS-Nr.	SL1210000

Gefahreninformationscode (GHS)

4-HYDROXYTAMOXIFEN Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R20/21/22:Gesundheitsschädlich beim Einatmen,Verschlucken und Berührung mit der Haut.
R63:Kann das Kind im Mutterleib möglicherweise schädigen.
S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S23:Gas/Rauch/Dampf/Aerosol nicht einatmen(geeignete Bezeichnung(en) vom Hersteller anzugeben).
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Chemische Eigenschaften
Powder
Verwenden
(Z)-4-Hydroxy Tamoxifen is a metabolite of Tamoxifen (T006000). (Z)-4-Hydroxy Tamoxifen is a hydroxylated analogue of Tamoxifen. (Z)-4-Hydroxy Tamoxifen is a metabolite of Tamoxifen with anti-estrogenic properties.
Verwenden
tamoxifen metabolite, anti-estrogen, see Tamoxifen 1,01038
Verwenden
A metabolite of Tamoxifen (T006000). A hydroxylated analogue of Tamoxifen with anti-estrogenic properties.
Verwenden
A hydroxylated analogue of tamoxifen with anti-estrogenic properties. A metabolite of Tamoxifen.
Definition
ChEBI: Afimoxifene is a tertiary amino compound that is tamoxifen in which the phenyl group which is in a Z- relationship to the ethyl substituent is hydroxylated at the para- position. It is the active metabolite of tamoxifen. It has a role as an antineoplastic agent, an estrogen receptor antagonist and a metabolite. It is a tertiary amino compound and a member of phenols. It is functionally related to a tamoxifen.
Allgemeine Beschreibung
A cell-permeable, active metabolite of Tamoxifen (Cat. No. 579000) that acts as a potent inhibitor of PKC. It is more potent than the parent compound and inhibits PKC by modifying its catalytic domain. Also available as a 10 mM solution in EtOH (Cat. No. 508225).
Biologische Aktivität
estrogen receptors (er) are members of the superfamily of ligand-modulated nuclear receptors that mediate the actions of steroid hormones, vitamin d, retinoids, and thyroid hormones. er is activated in vivo when bound by naturally occurring estrogens such as 17α-estradiol. in addition to regulating these physiological processes, estrogen also plays a central role in stimulating breast cancer growth. (z)-tamoxifen is a first generation selective er modulators that is currently approved by the fda and is widely used to treat estrogen-dependent breast cancers. its active metabolite, (z)-4-hydroxytamoxifen, is a potent estrogen receptor modulator.
Biochem/physiol Actions
Cell permeable: yes
in vitro
(z)-4-hydroxytamoxifen binds to er with 8-fold higher affinity than tamoxifen. it was found that only the z isomer has the required antiestrogenic activity; the (e)-4-hydroxytamoxifen has only about 5% of its affinity for the er [1].
in vivo
the antioestrogenic activities of (z)-4-hydroxytamoxifen and tamoxifen were determined after oral administration. (z)-4-hydroxytamoxifen was administered to groups of immature rats which also received s.c. injections of 0-2 μg oestradiol. both compounds produced a dose-related decrease in uterine wet weight when compared with the oestradiol-treated controls. at a dose of 1 μg/day, the antiuterotrophic effects of (z)-4-hydroxytamoxifen and tamoxifen were not significantly different but at 5μg/day, (z)-4-hydroxytamoxifen was more active (p < 0.01). (z)-4-hydroxytamoxifen therefore appears to retain its potent antioestrogenic activity after oral administration [2].
Lager
-20°C
Einzelnachweise
[1] donna d. yu and barry m. forman. simple and efficient production of (z)-4-hydroxytamoxifen, a potent estrogen receptor modulator. j. org. chem. 2003, 68, 9489-9491
[2] jordan vc, collins mm, rowsby l, prestwich g. a monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity. j endocrinol. 1977 nov;75(2):305-16.

4-HYDROXYTAMOXIFEN Upstream-Materialien And Downstream Produkte

4-HYDROXYTAMOXIFEN Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

68047-06-3, 4-HYDROXYTAMOXIFEN Verwandte Suche:

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