| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T408067-1ml |
1ml |
现货  |
|
| 英文别名 | (Z)-Tamoxifen, trans-Tamoxifen | (Z)-2-(4-(1,2-diphenylbut-1-enyl)phenoxy)-N,N-dimethylethanamine |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Tamoxifen (ICI 46474) |
| 生化机理 | 他莫昔芬（ICI 46474，(Z)-他莫昔芬，反式-他莫昔芬）是一种选择性雌激素受体调节剂（SERM）。他莫昔芬能增强 Hsp90 分子伴侣 ATP 酶的活性。他莫昔芬可诱导细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
Tamoxifen is a selective estrogen response modifier (SERM), protein kinase C inhibitor and anti-angiogenetic factor. Tamoxifen is a prodrμg 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 organs91. It has also been used to study its effect on lipopolysaccharide (LPS)-induced microglial activation92. Information Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selectiveestrogen receptormodulator (SERM). Tamoxifen enhances theHsp90molecular chaperoneATPaseactivity. Tamoxifen inducesapoptosis. TAM treatment inhibits significantly MCF7 cell proliferation. Low doses of TAM are able to induce structural chromosomal aberrations (deletions, isochromosomes, translocations, and dicentric chromosomes) in both ER+ and ER- breast cancer cells. This genotoxic effect is higher in those cell lines with HER2 gene amplification. Whereas TAM at lower concentrations (0.1-1 μM) induces a cell-cycle arrest, pharmacological concentrations (above 5 μM) of TAM have been found to induce apoptosis of breast cancer cells. 5 μM TAM rapidly induced sustained activation of ERK1/2 in ER-positive breast cancer cell lines (MCF-7 and T47D) In vivo Tamoxifen (TAM) is widely used for both treatment and prevention of breast cancer. However, it is also carcinogenic in human uterus and rat liver. Tm-inducible Cre-loxP systems are being used in broad areas of research and are providing important biologic insights in tissue development, maintenance, and function. Tamoxifen-induced nuclear localization of Cre recombinase is time- and dose-dependent. Higher doses of tamoxifen induce recombination weeks following administration and Lower doses of tamoxifen induce recombination up to one week following administration. Duration of tamoxifen-induced gene recombination is also dose-dependent. Administration of high Tm doses leads to extended CreER nuclear localization. Tm treatment induces side effects that may have physiologic consequences in Tm-inducible models. cell lines：CLL B cells or healthy volunteer T cells or NK cells Concentrations：10-6\u2009mol/L Incubation Time：24, 48, and 96\u2009h Powder Purity:≥99% |
| Canonical SMILES | CC/C(C1=CC=CC=C1)=C(C2=CC=CC=C2)/C3=CC=C(OCCN(C)C)C=C3.OC(=O)CC(O)(CC(O)=O)C(O)=O |
|---|---|
| 分子量 | 371.51 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 31 mg/mL (198.37 mM); Ethanol: 31 mg/mL (198.37 mM); Water: 16 mg/mL (102.38 mM); |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to Structure |
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