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

體外研究(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

體內(nèi)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

Animal Model:Aldh1l1-cre/ERT2 x Ai95 mice

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.

中文名稱

他莫昔芬；三苯氧胺；它莫西芬

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere

儲(chǔ)存方式

4°C, protect from light

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

溶解性數(shù)據(jù)

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

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨?。以下溶解方案都?qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

• 1.

  
  

  請(qǐng)依序添加每種溶劑： corn oil

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

  
  

• 2.

  
  

  請(qǐng)依序添加每種溶劑： 30% PEG400  0.5% Tween80  5% Propanediol  64.5%H2O

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

  
  

• 3.

  
  

  請(qǐng)依序添加每種溶劑： 10% EtOH    40% PEG300    5% Tween-80    45% saline

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

  
  

• 4.

  
  

  請(qǐng)依序添加每種溶劑： 10% EtOH    90% corn oil

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

  
  

• 5.

  
  

  請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% saline

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

  
  

• 6.

  
  

  請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

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

  
  

• 7.

  
  

  請(qǐng)依序添加每種溶劑： 10% DMSO    90% corn oil

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

  
  

• 8.

  
  

  請(qǐng)依序添加每種溶劑： 5% DMSO    40% PEG300    5% Tween-80    50% saline

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

  
  

• 9.

  
  

  請(qǐng)依序添加每種溶劑： 5% DMSO    95% (20% SBE-β-CD in saline)

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

參考文獻(xiàn)

[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.

Data Sheet

https://file.medchemexpress.cn/batch_PDF/HY-13757A/Tamoxifen-DataSheet-MedChemExpress.pdf