Tamoxifen(Synonyms: 他莫昔芬; ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen)

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Tamoxifen (Synonyms: 他莫昔芬; ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen) 纯度: 99.92%

Tamoxifen (ICI 47699) 是一种口服有效的,选择性雌激素受体 (estrogen receptor) 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 是一种有效的 Hsp90 激活剂,可增强 Hsp90 分子伴侣 ATPase 的活性。Tamoxifen 还可以有效抑制传染性 EBOV ZaireMarburg (MARV)IC50 分别为 0.1 µM 和 1.8 µM。Tamoxifen 可以激活自噬 (autophagy),诱导凋亡 (apoptosis)。Tamoxifen 还可以诱导 CreER(T2) 转基因小鼠的基因敲除。

Tamoxifen(Synonyms: 他莫昔芬; ICI 47699;  (Z)-Tamoxifen;  trans-Tamoxifen)

Tamoxifen Chemical Structure

CAS No. : 10540-29-1

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生物活性

Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[1][2][3]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively[5]. Tamoxifen activates autophagy and induces apoptosis[4]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[6].

IC50 & Target[1][4]

Estrogen receptor

 

HSP90

 

体外研究
(In Vitro)

Tamoxifen (ICI 47699) 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[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Injection of pre-mutant mice with Tamoxifen (75 mg/kg; injected for 5 days at 6 weeks of age) results in the excision of the floxed exon and, thus, in a gene knockout[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Aldh1l1-cre/ERT2 x Ai95 mice[3]
Dosage: 75 mg/kg
Administration: Injected for 5 days at 6 weeks of age
Result: Resulted in the excision of the floxed exon and a gene knockout.

Clinical Trial

分子量

371.51

Formula

C26H29NO

CAS 号

10540-29-1

中文名称

他莫昔芬;三苯氧胺;它莫西芬

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (168.23 mM; ultrasonic and warming and heat to 60°C)

Ethanol : 50 mg/mL (134.59 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6917 mL 13.4586 mL 26.9172 mL
5 mM 0.5383 mL 2.6917 mL 5.3834 mL
10 mM 0.2692 mL 1.3459 mL 2.6917 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: corn oil

    Solubility: 40 mg/mL (107.67 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 30% PEG400  0.5% Tween80  5% Propanediol  64.5%H2O

    Solubility: 5 mg/mL (13.46 mM); Suspended solution; Need ultrasonic

  • 3.

    请依序添加每种溶剂: 10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.73 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.73 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 4.

    请依序添加每种溶剂: 10% EtOH    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.73 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中,混合均匀。

  • 5.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.60 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.60 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 6.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (5.60 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.60 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 7.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.60 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.60 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 8.

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 0.83 mg/mL (2.23 mM); Clear solution

  • 9.

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: 0.83 mg/mL (2.23 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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]. Feil S, et, al. Inducible Cre mice. Methods Mol Biol. 2009;530:343-63.

    [7]. Laura Cooper, et al. Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem. 2020 Sep 4.

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