Endoxifen HCl
- Product Name
- Endoxifen HCl
- CAS No.
- 1032008-74-4
- Chemical Name
- Endoxifen HCl
- Synonyms
- CS-1633;Endoxifen HCl;Endoxifen Z-isomer HCl;Z-Endoxifen Hydrochloride;Endoxifen (hydrochloride);Endoxifen (Z-isomer hydrochloride);4-[(Z)-1-[4-[2-(methylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol,hydrochloride;(Z)-4-(1-(4-(2-(Methylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol hydrochloride
- CBNumber
- CB63040786
- Molecular Formula
- C25H28ClNO2
- Formula Weight
- 409.95
- MOL File
- 1032008-74-4.mol
Endoxifen HCl Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: 12.5 mg/mL (30.49 mM); Water: < 0.1 mg/mL (insoluble)
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- CS-5098
- Product name
- EndoxifenZ-isomerhydrochloride
- Purity
- 99.31%
- Packaging
- 1mg
- Price
- $90
- Updated
- 2021/12/16
- Product number
- CS-5098
- Product name
- EndoxifenZ-isomerhydrochloride
- Purity
- 99.31%
- Packaging
- 5mg
- Price
- $160
- Updated
- 2021/12/16
- Product number
- CS-5098
- Product name
- EndoxifenZ-isomerhydrochloride
- Purity
- 99.31%
- Packaging
- 10mg
- Price
- $280
- Updated
- 2021/12/16
- Product number
- orb611538
- Product name
- Endoxifen hydrochloride
- Packaging
- 100mg
- Price
- $615.4
- Updated
- 2021/12/16
- Product number
- DC8403
- Product name
- EndoxifenHCl
- Purity
- >98%
- Packaging
- 250mg
- Price
- $900
- Updated
- 2021/12/16
Endoxifen HCl Chemical Properties,Usage,Production
Uses
Endoxifen Z-isomer hydrochloride is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen inhibits hERG tail currents at 50 mV in a concentration-dependent manner with IC50 values of 1.6 μM. IC50 value: 1.6 μM [1] Target: hERG Potassium Channel, Estrogen Receptor/ERR Endoxifen is considered a prodrug, since it has a much higher potency for the estrogen receptor than its parent drug. Endoxifen inhibits the hERG channel protein trafficking to the plasma membrane in a concentration-dependent manner with Endoxifen being more potent than Tamoxifen. [1] Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen observed in Tamoxifen treated patients with deficient CYP2D6 activity (20 to 40 nM) markedly inhibit estrogen-induced cell proliferation rates in the presence of ERβ, whereas much higher Endoxifen concentrations are needed when ERβ is absent.[2]
Biological Activity
Endoxifen Z-isomer hydrochloride, as the active metabolite of Tamoxifen, is a potent and selective estrogen receptor antagonist.
target
| Target | Value |
| Estrogen receptor |
References
[1] Chae YJ, et al. Endoxifen, the active metabolite of tamoxifen, inhibits cloned hERG potassium channels. Eur J Pharmacol. 2015 Apr 5;752:1-7. DOI:10.1016/j.ejphar.2015.01.048
[2] Wu X, et al. Estrogen receptor-beta sensitizes breast cancer cells to the anti-estrogenic actions of endoxifen. Breast Cancer Res. 2011 Mar 10;13(2):R27. DOI:10.1186/bcr2844
Endoxifen HCl Preparation Products And Raw materials
Raw materials
Preparation Products
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