他莫昔芬/三苯氧胺/Tamoxifen/三苯氧胺,≥99%
- 产品编号：T0120
- 中文名称：他莫昔芬/三苯氧胺/Tamoxifen/三苯氧胺
- 英文名称：Tamoxifen
- 英文别名:(Z)-1-(p-Dimethylaminoethoxyphenyl)-1,2-diphenyl-1-butene, trans-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine
- CAS号:10540-29-1
- 分子式:C6H5C(C2H5)=C(C6H5)C6H4OCH2CH2N(CH3)2
- 分子量:371.51
- 纯度:≥99%
- EC号:234-118-0
- MDL号:MFCD00010454
订货信息：
产品规格价格(RMB)
- T0120-50MG150
- T0120-100MG260
- T0120-1G2200
性能描述
| 试剂纯度 |
≥99% |
| mp |
97-98 °C(lit.) |
| storage temp. |
2-8°C |
Tamoxifen is a selective estrogen response modifier (SERM), protein kinase C inhibitor and anti-angiogenetic factor. Tamoxifen 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.
Biochem/physiol Actions
Protein kinase C inhibitor. 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.
用途：
1、该药为雌二醇竞争性拮抗剂，能与乳腺细胞的雌激素受体结合，不刺激转录或作用微弱。药物-受体复合物不易解离，组织受体的循环应用，也是作用机制之一。他莫昔芬能上调转化生长因子β生成，此因子减少与恶性肿瘤的发展有关。还对蛋白激酶C有特异性抑制作用。这些作用都对依赖雌激素才能继续生长的肿瘤细胞有抑制作用。多用于绝经期前雌激素（ER+）和孕激素受体（PR+）呈进行性发展的乳癌的治疗。他莫昔芬对血浆脂代谢、子宫内膜和骨的作用则仍是雌激素性质，不呈拮抗作用。他莫昔芬的抗骨质疏松作用也可能与上调转化生长因子β有关，因为此因子能够控制成骨细胞和破骨细胞间的平衡。
2、可以作为基因敲除基础的一个研究工具，可以构建条件敲除小鼠模型，调节特定基因表达表达或不表达。
