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

Endoxifen  (Synonyms: 因多昔芬)

目錄號: HY-18719E 純度: 99.42%
COA 產品使用指南 技術支持

Endoxifen 是 Tamoxifen 的關鍵活性代謝物,與雌激素受體 (estrogen receptor) 有較高的親和力和特異性,同時也能抑制芳香酶的活性。Endoxifen 有用于乳腺癌研究的潛力。

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Endoxifen Chemical Structure

Endoxifen Chemical Structure

CAS No. : 110025-28-0

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥547
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5 mg ¥498
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10 mg ¥800
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50 mg ¥2800
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100 mg ¥4500
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500 mg   詢價  

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Customer Review

MCE 顧客使用本產品發(fā)表的 1 篇科研文獻

  • 生物活性

  • 實驗參考方法

  • 純度 & 產品資料

  • 參考文獻

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

 

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
HeLa IC50
3.05 μM
Compound: Endoxifen
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
[PMID: 29624387]
MCF-10A IC50
> 10 μM
Compound: Endoxifen
Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability after 72 hrs by cell counter method
Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability after 72 hrs by cell counter method
[PMID: 34364162]
MCF7 IC50
0.1 μM
Compound: Endoxifen
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by cell counter method
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by cell counter method
[PMID: 34364162]
體外研究
(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.

體內研究
(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 號
性狀

固體

顏色

White to light yellow

中文名稱

因多昔芬

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 62.5 mg/mL (167.34 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質量 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
查看完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內使用,-20°C儲存時,請在1個月內使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結果
工作液所需濃度 : mg/mL
純度 & 產品資料
參考文獻
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.

參考文獻

完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內使用,-20°C儲存時,請在1個月內使用。

可選溶劑 濃度 溶劑體積 質量 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.

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產品名稱:
Endoxifen
目錄號:
HY-18719E
需求量: