2. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Anti-infection
  3. Cytochrome P450 Estrogen Receptor/ERR Drug Metabolite Parasite
  4. Endoxifen

Endoxifen  (Synonyms: 因多昔芬)

目录号: HY-18719E 纯度: 99.42%
COA 产品使用指南

摩尔计算器

Endoxifen 是 Tamoxifen 的关键活性代谢物，与雌激素受体 (estrogen receptor) 有较高的亲和力和特异性，同时也能抑制芳香酶的活性。Endoxifen 有用于乳腺癌研究的潜力。

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Endoxifen Chemical Structure

Endoxifen Chemical Structure

CAS No. : 110025-28-0

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规格 价格 是否有货 数量
5 mg ￥498
In-stock
10 mg ￥800
In-stock
50 mg ￥2800
In-stock
100 mg ￥4500
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Endoxifen:

Endoxifen 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

查看 Estrogen Receptor/ERR 亚型特异性产品:

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

查看 Parasite 亚型特异性产品:

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study[1][2].

IC50 & Target[2]

Aromatase

 

ERα

 

体外研究
(In Vitro)

Endoxifen, a hydroxylated Tamoxifen metabolite, is approximately 100-fold more potent as an antagonist of the ER than tamoxifen. It also suggests that endoxifen but not 4-hydroxytamoxifen results in ER-alpha degradation in addition to its effects on the ER at the level of transcription[1]. Endoxifen, is a potent antiestrogen that targets estrogen receptor α for degradation in breast cancer cells. Additionally, it is showed that Endoxifen blocks ERA transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation even in the presence of tamoxifen, N-desmethyl-tamoxifen, and 4-hydroxytamoxifen[2]. Endoxifen is strongly growth inhibitory at 10 μM for all the breast cancer cell lines except for moderate inhibition for MDAMB-468.Cytotoxic effects are quite significant at 10 μM concentration for MCF7, HS 578T, and BT-549 cells. At lower Endoxifen concentrations (0.01-1 μM), the inhibitory effects are not as significant as 10 μM, whereas 100 μM Endoxifen concentration found to be lethal for all tested cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Endoxifen 相关抗体:
体内研究
(In Vivo)

Orally administered Endoxifen is rapidly absorbed and systemically available when tested in female rats. The Endoxifen-treated rats show 787% higher exposure (AUC0–∞) and 1,500% higher concentration (Cmax) levels of Endoxifen when compared with Tamoxifen. Oral Endoxifen administration once a day for 28 consecutive days at dosages 2, 4, and 8 mg/kg proves safe and results in progressive inhibition of the growth of the human mammary tumor xenografts in female mice[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

373.49

Formula

C25H27NO2
CAS 号
性状

固体

颜色

Off-white to light yellow

中文名称

因多昔芬
运输条件

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

DMSO 中的溶解度 : 66.67 mg/mL (178.51 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6774 mL 13.3872 mL 26.7745 mL
5 mM 0.5355 mL 2.6774 mL 5.3549 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Animal Administration
[2]

Mice[2]
Six-weeks-old, female, athymic NCr–nu/nu mice are implanted subcutaneously (s.c.) near the right flank with 30-40-mg fragment of MCF-7 human mammary tumor from an in vivo passage. The day of tumor fragments implantation is designated as Day 0. To support the estrogen-dependent MCF-7 tumor growth, each animal is implanted s.c. in the back of the neck with a 0.72-mg 17 β-estradiol 60-day release pellet 1 day prior to tumor fragment implantation. Individual tumors grew to 75-196 mm3 in size on Day 13 after tumor fragment implantation, the day of treatment initiation. A total of 36 tumor bearing mice are randomized and divided into 4 treatments (6 mice/group) and one control (12 mice/group) groups. At day 13 post tumor implantation, treatment with control (water), Endoxifen at three dose levels (2, 4, and 8 mg/kg) or Tamoxifen twice a day, 3 h apart at a dosage of 10 mg/kg are administered by oral gavage once daily for 28 consecutive days. The dose volume 0.2 mL/10 g body weight is kept constant for all treatment groups. The s.c. tumors are measured and the animals are weighed twice weekly starting on the first day of treatment. The study is terminated on Day 58. The median time to reach two tumor mass doublings is used in the calculation of the overall delay in the growth of the median tumor. Additionally, comparison of the median tumor weight in the treatment groups to the median tumor weight in the control group (T/C 9 100%) on Day 41 (1 day after the last treatment) and on Day 58 (the day of study termination) are used for an additional evaluation of the antitumor efficacy[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Endoxifen 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6774 mL 13.3872 mL 26.7745 mL 66.9362 mL
5 mM 0.5355 mL 2.6774 mL 5.3549 mL 13.3872 mL
10 mM 0.2677 mL 1.3387 mL 2.6774 mL 6.6936 mL
15 mM 0.1785 mL 0.8925 mL 1.7850 mL 4.4624 mL
20 mM 0.1339 mL 0.6694 mL 1.3387 mL 3.3468 mL
25 mM 0.1071 mL 0.5355 mL 1.0710 mL 2.6774 mL
30 mM 0.0892 mL 0.4462 mL 0.8925 mL 2.2312 mL
40 mM 0.0669 mL 0.3347 mL 0.6694 mL 1.6734 mL
50 mM 0.0535 mL 0.2677 mL 0.5355 mL 1.3387 mL
60 mM 0.0446 mL 0.2231 mL 0.4462 mL 1.1156 mL
80 mM 0.0335 mL 0.1673 mL 0.3347 mL 0.8367 mL
100 mM 0.0268 mL 0.1339 mL 0.2677 mL 0.6694 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Endoxifen110025-28-0因多昔芬Cytochrome P450Estrogen Receptor/ERRDrug MetaboliteParasiteCYPsInhibitorinhibitorinhibit

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