Tamoxifen, white powder
Supplier: TestTotal Ratings: 0
Avg. Ratings: 0.0 out of 5
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Danger
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Protein kinase C inhibitor (IC50 = 50-200 µM depending on assay conditions in MCF-7 cells or IC50 = 100 µM in rat brain). The PKC inhibition is also dependent on the phosopholipid concentration. Also inhibits both calmodulin-dependent and calmodulin-independent Ca2+-, Mg2+-ATPase. Tamoxifen is a selective estrogen response modifier (SERM), anti-angiogenetic factor. It is a prodrug that is metabolized to active metabolites 4-hydroxytamoxifen (4-OHT) and endoxifen by cytochrome P450 isoforms CYP2D6 and CYP3A4. In breast cancer, the gene repressor activity of tamoxifen against ERBB2 is dependent upon PAX2. Blocks estradiol-stimulated VEGF production in breast tumor cells.
Tamoxifen has been used to facilitate the recombination of ect2flox allele in mouse organs. It has also been used to study its effect on lipopolysaccharide (LPS)-induced microglial activation
Tamoxifen is a Protein kinase C inhibitor. It induces apoptosis in human malignant glioma cell lines. Tamoxifen and its metabolite 4-hydroxytamoxifen are selective estrogen response modifiers (SERMs) that act as estrogen antagonists in mammary gland. Blocks estradiol-stimulated VEGF production in breast tumor cells.
- Presentation: White Powder
- pKa: approximately 8.85; approximately 6.9 (in Triton® X-100)
- Practically insoluble in water (< 0.01% at 20 °C); soluble in methanol, ethanol, 2-propanol, propylene glycol, chloroform (50 mg/mL - clear, colorless to faint yellow solution) or DMSO.
- Storage temperature: Store at +4 °C.
Tamoxifen has been shown to protect bone from estrogen-deficiency bone loss and lower plasma cholesterol in the rat. A 10 µM solution has exhibited fungicidal activity (optimal pH 7.5) against yeast cells of C. albicans. It has been implemented in liver carcinogenesis in rats. A possible mechanism for the DNA adduct formation leading to carcinogenesis was reported. 100 nM solutions combined with vinblastine are cytotoxic to both rat prostate adenocarcinoma cell line and human prostate cancer cells. Flow cytometric analysis of DNA content and BrdU (5-bromo-2'-deoxyuridine) labeling in MCF-7 (estrogen-responsive human clonal breast cancer cell line) cells have shown that the effect of tamoxifen on the growth of estrogen-dependent cells in culture may be due to accumulation of cells in G1 phase (before onset of S-phase) and the exit of some cells from the cycling compartment in the cell cycle progress. The mechanism of tamoxifen action may involve interactions in the signaling transduction pathway: tamoxifen is a competitive inhibitor of calmodulin-stimulated phosphodiesterase activity; molecular interactions between tamoxifen and calmodulin were reported.
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Specification Test Results
| Identity Test | Passes |
| Melting Point | 96-100°C |
| FTIR | Conforms to Standard |
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