- 4-HYDROXYTAMOXIFEN
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- $1.00
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2019-09-02
- CAS:68047-06-3
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 1lg; 2kg; 5kg; 10kg; 100kg
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| | 4-HYDROXYTAMOXIFEN Basic information |
| | 4-HYDROXYTAMOXIFEN Chemical Properties |
| Melting point | 105-107°C | | Boiling point | 513.45°C (rough estimate) | | density | 1.1005 (rough estimate) | | refractive index | 1.6000 (estimate) | | storage temp. | 2-8°C | | solubility | 95% ethanol: 20 mg/mL | | form | powder | | pka | 10.35±0.15(Predicted) | | color | white | | Stability: | Stable. Store cool. Incompatible with strong oxidizing agents. | | InChI | InChI=1S/C26H29NO2/c1-4-25(20-8-6-5-7-9-20)26(21-10-14-23(28)15-11-21)22-12-16-24(17-13-22)29-19-18-27(2)3/h5-17,28H,4,18-19H2,1-3H3/b26-25- | | InChIKey | TXUZVZSFRXZGTL-OCEACIFDSA-N | | SMILES | C1(O)=CC=C(/C(/C2=CC=C(OCCN(C)C)C=C2)=C(/C2=CC=CC=C2)\CC)C=C1 | | CAS DataBase Reference | 68047-06-3 |
| Hazard Codes | Xn | | Risk Statements | 20/21/22-63 | | Safety Statements | 22-23-36 | | WGK Germany | 3 | | RTECS | SL1210000 | | Storage Class | 6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects | | Hazard Classifications | Acute Tox. 4 Oral
Aquatic Acute 1
Aquatic Chronic 1
Carc. 1B
Repr. 1B |
| | 4-HYDROXYTAMOXIFEN Usage And Synthesis |
| Chemical Properties | Powder | | Uses | A hydroxylated analogue of tamoxifen with anti-estrogenic properties. A metabolite of Tamoxifen. | | Uses | A metabolite of Tamoxifen (T006000). A hydroxylated analogue of Tamoxifen with anti-estrogenic properties. | | Uses | (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. | | Uses | tamoxifen metabolite, anti-estrogen, see Tamoxifen 1,01038 | | 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. | | General Description | 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). | | Biological Activity | 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]. | | storage | -20°C | | references | [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 Preparation Products And Raw materials |
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