标签归档：tamoxifen

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

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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 Zaire 和 Marburg (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

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥550 In-stock
500 mg ￥500 In-stock
1 g ￥690 In-stock
5 g ￥2750 In-stock
10 g ￥3500 In-stock
50 g   询价  

* Please select Quantity before adding items.

Tamoxifen 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Metabolism/Protease Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • Endoplasmic Reticulum Stress Compound Library
  • Pyroptosis Compound Library
  • Cytoskeleton Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Targeted Therapy Drug Library
  • Tumorigenesis Related Compound Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Tamoxifen Citrate(Synonyms: 他莫昔芬柠檬酸盐; ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Tamoxifen Citrate (Synonyms: 他莫昔芬柠檬酸盐; ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate) 纯度: 99.93%

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(Synonyms: 他莫昔芬柠檬酸盐; ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate)

Tamoxifen Citrate Chemical Structure

CAS No. : 54965-24-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥550 In-stock
500 mg ￥500 In-stock
1 g ￥690 In-stock
5 g ￥2750 In-stock
10 g   询价  
50 g   询价  

* Please select Quantity before adding items.

Tamoxifen Citrate 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Metabolism/Protease Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • Endoplasmic Reticulum Stress Compound Library
  • Pyroptosis Compound Library
  • Cytoskeleton Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Tumorigenesis Related Compound Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

生物活性

Tamoxifen Citrate (ICI 46474) 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 Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively[5]. Tamoxifen Citrate activates autophagy and induces apoptosis[4].

IC50 & Target

HSP90

 

Estrogen receptor

 

体外研究
(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[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)

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[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.
Clinical Trial

分子量

563.64

Formula

C32H37NO8
CAS 号

54965-24-1
中文名称

他莫昔芬柠檬酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (88.71 mM; Need ultrasonic)

Ethanol : 10 mg/mL (17.74 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7742 mL 8.8709 mL 17.7418 mL
5 mM 0.3548 mL 1.7742 mL 3.5484 mL
10 mM 0.1774 mL 0.8871 mL 1.7742 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 (sealed storage, away from moisture)。-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: 10 mg/mL (17.74 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.69 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

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.69 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 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
  • 4.

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

    Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.69 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。

*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]. Jia Y, et al. Cardiomyocyte-Specific Ablation of Med1 Subunit of the Mediator Complex Causes Lethal DilatedCardiomyopathy in Mice. PLoS One. 2016 Aug 22;11(8):e0160755.

    [4]. Zhao R, et al. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. PLoS One. 2010 Apr 1;5(4):e9934.

    [5]. Laura Cooper, et al. Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem. 2020 Sep 4.
Animal Administration
[3]

Mice[3]
Seven-week old TmcsMed1-/- mice and the wild-type littermates are then administered Tamoxifen intraperitoneally at a daily dose of 65 mg/kg body weight for 5 days and then killed at selected intervals after initiation of Tamoxifen treatment. For each experiment 3 to 5 mice for control and csMed1-/- are used. To obtain survival curve 41 csMed1-/- and 41 csMed1fl/fl mice are used. Thirteen TmcsMed-/- mice and the same number of littermates are used for the survival curve experiments using Tamoxifen inducible model.

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.
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]. Jia Y, et al. Cardiomyocyte-Specific Ablation of Med1 Subunit of the Mediator Complex Causes Lethal DilatedCardiomyopathy in Mice. PLoS One. 2016 Aug 22;11(8):e0160755.

    [4]. Zhao R, et al. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. PLoS One. 2010 Apr 1;5(4):e9934.

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

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Tamoxifen-​d5(Synonyms: ICI 47699-​d5; (Z)-Tamoxifen-​d5; trans-Tamoxifen-​d5)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Tamoxifen-​d5 (Synonyms: ICI 47699-​d5; (Z)-Tamoxifen-​d5; trans-Tamoxifen-​d5)

Tamoxifen-d5 (ICI 47699-d5) 是一种 Tamoxifen 氘代物。Tamoxifen (ICI 47699) 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 是一种有效的 Hsp90 激活剂，可增强 Hsp90 分子伴侣 ATPase 的活性。

Tamoxifen-​d5(Synonyms: ICI 47699-​d5; (Z)-Tamoxifen-​d5; trans-Tamoxifen-​d5)

Tamoxifen-​d5 Chemical Structure

CAS No. : 157698-32-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity[1][2].

IC50 & Target

Estrogen receptor

 

HSP90

 

分子量

376.55

Formula

C26H24D5NO
CAS 号

157698-32-3
中文名称

他莫昔芬 ​d5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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]. Zhao R, et al. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. PLoS One. 2010 Apr 1;5(4):e9934.

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α-Hydroxytamoxifen(Synonyms: (E)-α-Hydroxy tamoxifen; α-OHTAM)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

α-Hydroxytamoxifen (Synonyms: (E)-α-Hydroxy tamoxifen; α-OHTAM)

α-Hydroxytamoxifen 是 tamoxifen 的代谢物，在没有代谢酶的条件下可与 DNA 相互反应，并导致 DNA 加合物的形成。

α-Hydroxytamoxifen(Synonyms: (E)-α-Hydroxy tamoxifen; α-OHTAM)

α-Hydroxytamoxifen Chemical Structure

CAS No. : 97151-02-5

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生物活性

α-Hydroxytamoxifen is a metabolite of tamoxifen, reacts with DNA in the absence of metabolizing enzymes, and causes formation of DNA adducts[1].

分子量

387.51

Formula

C26H29NO2
CAS 号

97151-02-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Phillips DH, et al. alpha-Hydroxytamoxifen, a metabolite of tamoxifen with exceptionally high DNA-binding activity in rat hepatocytes. Cancer Res. 1994 Nov 1;54(21):5518-22.

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N-Desmethyltamoxifen

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

N-Desmethyltamoxifen 

N-Desmethyltamoxifen 是 Tamoxifen 在人体内的主要代谢产物。N-Desmethyltamoxifen，较弱的抗雌激素，是一种比 Tamoxifen 强十倍的蛋白激酶 C (PKC) 抑制剂。N-Desmethyltamoxifen 也是人体 AML 细胞神经酰胺代谢的有效调节因子，限制神经酰胺糖基化、水解和鞘氨醇磷酸化。

N-Desmethyltamoxifen

N-Desmethyltamoxifen Chemical Structure

CAS No. : 31750-48-8

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N-Desmethyltamoxifen 的其他形式现货产品:

N-Desmethyltamoxifen hydrochloride

生物活性

N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation[1][2][3].

IC50 & Target[1][2]

PKC

 

Estrogen Receptor

 

Human Endogenous Metabolite

 

体外研究
(In Vitro)

N-desmethyltamoxifen (20-500 ng/ml; 48 hours) has a profound inhibitory effect upon all seven glioma lines (T98G, U87, U138, U373, ALW, AUK, CAS cells)[1].
N-desmethyltamoxifen (1.5-10 μM; 114 hours) inhibits growth of MCF 7 human mammary carcinoma cells[2].
N-desmethyltamoxifen, resulting from the CYP3A4/5-mediated catalysis of tamoxifen, is the major primary quantitative metabolite of tamoxifen[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: MCF 7 human mammary carcinoma cells
Concentration: 1.5, 2.5, 5, 7.5, 10 μM
Incubation Time: 114 hours
Result: Inhibits growth of MCF 7 human mammary carcinoma cells

分子量

357.49

Formula

C25H27NO
CAS 号

31750-48-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Vertosick FT Jr, et al. A comparison of the relative chemosensitivity of human gliomas to tamoxifen and n-desmethyltamoxifen in vitro. J Neurooncol. 1994;19(2):97-103.

    [2]. Morad SA, et al. Modification of sphingolipid metabolism by tamoxifen and N-desmethyltamoxifen in acute myelogenous leukemia–Impact on enzyme activity and response to cytotoxics. Biochim Biophys Acta. 2015 Jul;1851(7):919-28.

    [3]. Reddel RR,et al. N-desmethyltamoxifen inhibits growth of MCF 7 human mammary carcinoma cells in vitro. Eur J Cancer Clin Oncol. 1983 Aug;19(8):1179-81.

    [4]. Seong Hwan Kim,et al. Use of Antidepressants in Patients with Breast Cancer Taking Tamoxifen. J Breast Cancer. 2010 Dec;13(4):325-336.

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FLTX1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FLTX1  纯度: 99.71%

FLTX1 是一种荧光他莫昔芬 (Tamoxifen) 衍生物，可以在透化和非透化条件下特异性标记细胞内 Tamoxifen 结合位点 (雌激素受体)。FLTX1 在乳腺癌细胞中表现出 Tamoxifen 有效的抗雌激素特性。FLTX1 缺乏对子宫的雌激素激动作用。

FLTX1

FLTX1 Chemical Structure

CAS No. : 1481401-71-1

规格 价格 是否有货 数量
5 mg ￥4500 In-stock
10 mg ￥7500 In-stock
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FLTX1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Anti-Breast Cancer Compound Library

生物活性

FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus[1][2].

IC50 & Target

ERα

87.5 nM (IC50)

体外研究
(In Vitro)

FLTX1 (0.01-10 μM; 6 d) reduces MCF7 cell proliferation in a dose-dependent manner. FLTX1 (pretreated 24 h) counteracts the increase in cell growth induced by E2 down to the vehicle level[1].
FLTX1 (50 μM; 2 h) exhibits a dose-dependent competition with Tamoxifen (Tx) in MCF7 cells[1].
FLTX1 (0.1 nM-100 μM; 18 h) competitively displaces the [3H] E2 binding to rat uterine estrogen receptors (ER) rat uterus cytosol, with an IC50 of 87.5 nM[1].
FLTX1 (0.1 nM-10 μM; pretreated 8 h) reduces the estradiol-induced luciferase expression activity in a dose-dependent manner. FLTX1 (15-16 h) is devoid of the potent estrogenic agonist activity in both transiently transfected MCF7 cells and stably transfected T47D-KBluc cells[1].

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.

Cell Proliferation Assay[1]

Cell Line: MCF7 cells
Concentration: 0.01, 0.1, 1, 5, 10 μM
Incubation Time: 6 days
Result: Inhibited MCF7 cell proliferation in a dose-dependent manner, being significantly more effective than Tx already at 0.1 μM.

体内研究
(In Vivo)

FLTX1 (0.01-1 mg/kg/d; s.c. for 3 d) is lacked of the estrogenic uterotrophic (and also cervical and vaginal), hyperplasic and hypertrophic effects, and failed to alter basal proliferating cell nuclear antigen immunoreactivity in mice and rats[1].

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.
分子量

520.58

Formula

C31H28N4O4
CAS 号

1481401-71-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (48.02 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9209 mL 9.6047 mL 19.2093 mL
5 mM 0.3842 mL 1.9209 mL 3.8419 mL
10 mM 0.1921 mL 0.9605 mL 1.9209 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。-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。
参考文献

  • [1]. Marrero-Alonso J, et, al. Unique SERM-like properties of the novel fluorescent tamoxifen derivative FLTX1. Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):898-910.

    [2]. Morales A, et, al. Colocalization of Estrogen Receptors with the Fluorescent Tamoxifen Derivative, FLTX1, Analyzed by Confocal Microscopy. Methods Mol Biol. 2016;1366:163-173.

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