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

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.

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Endoxifen

Endoxifen 構造式

CAS 番号 : 110025-28-0

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 在庫あり
Solution
10 mM * 1 mL in DMSO USD 55 在庫あり
Solid
5 mg $50 在庫あり
10 mg $80 在庫あり
50 mg $280 在庫あり
100 mg $450 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

Other Forms of Endoxifen:

Endoxifen 関連抗体

Top Publications Citing Use of Products

Cytochrome P450 アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

Estrogen Receptor/ERR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Parasite アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

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製品説明

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

 

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
0.029 μM
Compound: Endoxifen
Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 24 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 24 hrs by MTT assay
[PMID: 38911170]
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]
体外実験

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].

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

Endoxifen 関連抗体
体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

373.49

分子式

C25H27NO2
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

CC/C(C1=CC=CC=C1)=C(C2=CC=C(O)C=C2)/C3=CC=C(OCCNC)C=C3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 62.5 mg/mL (167.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.2677 mL 1.3387 mL 2.6774 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

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体積 （終了）

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション

純度: 99.51%

COA (247 KB) HNMR (264 KB) LCMS (95 KB)

取扱説明書 (2659 KB)
参考文献
動物実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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Endoxifen Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

Endoxifen110025-28-0Cytochrome P450Estrogen Receptor/ERRDrug MetaboliteParasiteCYPsInhibitorinhibitorinhibit

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製品番号:
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