Tamoxifen枸橼酸他莫昔芬,54965-24-1

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Tamoxifen Citrate

CAS No. : 54965-24-1

MCE 国际站：Tamoxifen Citrate

产品活性：Tamoxifen Citrate (ICI 46474) 是一种口服有效的，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，肝脏和子宫细胞中的雌激素活性。Tamoxifen Citrate 是一种有效的 Hsp90 激活剂，可增强 Hsp90 分子伴侣 ATPase 的活性。Tamoxifen Citrate 还可以有效抑制传染性 EBOV Zaire 和 Marburg (MARV)，IC₅₀ 分别为 0.1 µM 和 1.8 µM。Tamoxifen Citrate 可以激活自噬 (autophagy)，诱导凋亡 (apoptosis)。Tamoxifen Citrate 还可以诱导 CreER(T2) 转基因小鼠的基因敲除。

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

In Vitro: Tamoxifen Citrate (ICI 46474) shows strong inhibition of MCF-7 cells (EC₅₀=1.41 μM) and to a lesser extent the T47D cells (EC₅₀=2.5 μM) but does not affect the MDA-MB-231 cells.

In Vivo: The Tamoxifen Citrate-inducible gene knockout strategy has clear advantages in that expression of a gene can be ablated in adult mice at will in a tissue specific manner. To study the role of Med1 in adult heart, 7-week old TmcsMed1^-/- mice are given a daily Iintraperitoneal injection of Tamoxifen Citrate at a dose of 65 mg/kg for 5 days and killed at selected intervals thereafter. qPCR analysis of RNA shows that the Med1 expression begin to decrease after 3 days of Tamoxifen Citrate injection (about 70% decrease), and by 5 days of injection, Med1 expression is almost non-detectable in the heart. Tamoxifen Citrate-inducible cardiac-specific disruption of Med1 (TmcsMed1^-/-) in adult mice causes dilated cardiomyopathy.

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