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MCE 国际站：Tamoxifen
中文名：他莫昔芬
CAS：10540-29-1
品牌：MedChemExpress (MCE)
存储条件：4°C, protect from light
生物活性：Tamoxifen (ICI 47699) 是一种具有口服活性的选择性雌激素受体调节剂 (SERM)，可阻断乳腺细胞中的雌激素作用，并可激活其他细胞（如骨骼）中的雌激素活性、肝脏和子宫细胞[1][2][3]。 Tamoxifen 是一种有效的 Hsp90 激活剂，可增强 Hsp90 分子伴侣 ATP 酶活性。他莫昔芬还有效抑制传染性 EBOV Zaire 和 Marburg (MARV)，IC50 分别为 0.1 μM 和 1.8 μM，分别[5]。他莫昔芬激活自噬并诱导细胞凋亡[4]。他莫昔芬还能诱导CreER(T2)转基因小鼠的基因敲除[6]。
体外：Tamoxifen (ICI 47699) 对 MCF-7 细胞 (EC50=1.41 μM) 表现出强烈的抑制作用，对 T47D 细胞 (EC50=2.5 μM) 的抑制作用较小，但不影响 MDA-MB-231 细胞[2]。
体内：向突变前小鼠注射他莫昔芬（75 mg/kg；在 6 周龄时注射 5 天）导致 floxed 外显子切除，从而导致基因敲除[3] .
热销产品：Gemcitabine | 4-Hydroxytamoxifen | Metformin | Obeticholic acid | MS67 | Sorafenib | Mitoquinone (mesylate) | Niraparib | Everolimus | Capsaicin
研究领域：Vitamin D Related/Nuclear Receptor | metabolic Enzyme/Protease | Cell Cycle/DNA Damage | Autophagy | Apoptosis
作用靶点：Estrogen Receptor/ERR | HSP | Autophagy | Apoptosis
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
参考文献：
[1]. Osborne CK. Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998 Nov 26;339(22):1609-18.
[2]. Hawariah A, et al. In vitro response of human breast cancer cell lines to the growth-inhibitory effects of styrylpyrone derivative (SPD) and assessment of its antiestrogenicity. Anticancer Res. 1998 Nov-Dec;18(6A):4383-6.
[3]. Jun Nagai, et al. Hyperactivity with Disrupted Attention by Activation of an Astrocyte Synaptogenic Cue. Cell. 2019 May 16;177(5):1280-1292.e20.
[4]. Zhao R, et al. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. PLoS One. 2010 Apr 1;5(4):e9934.
[5]. Kedjouar B, et al. Molecular characterization of the microsomal tamoxifen binding site. J Biol Chem. 2004 Aug 6;279(32):34048-61.
[6]. Laura Cooper, et al. Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem. 2020 Sep 4.
[7]. Feil S, et, al. Inducible Cre mice. Methods Mol Biol. 2009;530:343-63.
