Endoxifen
Based on 1 publication(s) in Google Scholar
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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- Pureza : 99.51%
- No. CAS: 110025-28-0
- Fòrmula: C25H27NO2
- Peso molecular:373.49
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-16950
4-HydroxytamoxifenEstrogen Receptor Modulator -
HY-13757A
TamoxifenEstrogen Receptor Modulator -
HY-50752
LY-411575γ-secretase Inhibitor -
HY-129099A
N-Desmethyltamoxifen hydrochloridePKC Inhibitor -
HY-12501A
ITI-214PDE1 Inhibitor -
HY-B0141A
Alpha-Estradiol5α-reductase Inhibitor -
HY-18719ER
Endoxifen (Standard) -
HY-14590
KaempferolEstrogen Receptor α Inhibitor -
HY-B0652
EtonogestrelProgesterone/ERR Agonist -
HY-14590R
Kaempferol (Standard) -
HY-B0845
ProchlorazAntifungal -
HY-B0554
NorethindroneProgestin
Publications Citing Use of MedChemExpress (MCE) Endoxifen
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Actividad biológica
Descripciòn
IC50 & Target
[2]|
Aromatase |
ERα |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
3.05 μM
Compound: Endoxifen
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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
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[PMID: 29624387] |
| MCF-10A | IC50 |
>10 μM
Compound: Endoxifen
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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
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[PMID: 34364162] |
| MCF7 | IC50 |
0.029 μM
Compound: Endoxifen
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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
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[PMID: 38911170] |
| MCF7 | IC50 |
0.1 μM
Compound: Endoxifen
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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
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[PMID: 34364162] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 110025-28-0
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Appearance Solid
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Peso molecular 373.49
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Fòrmula C25H27NO2
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Color White to light yellow
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SMILES
CC/C(C1=CC=CC=C1)=C(C2=CC=C(O)C=C2)/C3=CC=C(OCCNC)C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Antibiotics (Basel)
Efficacy of Tamoxifen Metabolites in Combination with Colistin and Tigecycline in Experimental Murine Models of Escherichia coli and Acinetobacter baumannii. [Abstract]2024 Apr 24;13(5):386. PMID: 38786115
Solvente y solubilidad
In Vitro:
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Goetz MP, et al. Tamoxifen, endoxifen, and CYP2D6: the rules for evaluating a predictive factor. Oncology (Williston Park). 2009 Dec;23(14):1233-4, 1236. [Content Brief]
[2]. Wu X, et al. The tamoxifen metabolite, endoxifen, is a potent antiestrogen that targets estrogen receptor alpha for degradation in breast cancer cells. Cancer Res. 2009 Mar 1;69(5):1722-7. [Content Brief]
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 |
Endoxifen Related Classifications
HY-18719E Related Classifications
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