Endoxifen (E-isomer hydrochloride)

Modify Date: 2024-01-28 17:04:23

Endoxifen (E-isomer hydrochloride) Structure
Endoxifen (E-isomer hydrochloride) structure
Common Name Endoxifen (E-isomer hydrochloride)
CAS Number 1197194-61-8 Molecular Weight 409.948
Density N/A Boiling Point N/A
Molecular Formula C25H28ClNO2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Endoxifen (E-isomer hydrochloride)


Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM). Target: Estrogen Receptor/ERREndoxifen 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]

 Names

Name 4-[(1E)-1-{4-[2-(Methylamino)ethoxy]phenyl}-2-phenyl-1-buten-1-yl]phenol hydrochloride (1:1)
Synonym More Synonyms

 Endoxifen (E-isomer hydrochloride) Biological Activity

Description Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM). Target: Estrogen Receptor/ERREndoxifen 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]
Related Catalog
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.

[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.

 Chemical & Physical Properties

Molecular Formula C25H28ClNO2
Molecular Weight 409.948
Exact Mass 409.180847
Storage condition 2-8℃

 Synonyms

4-[(1E)-1-{4-[2-(Methylamino)ethoxy]phenyl}-2-phenyl-1-buten-1-yl]phenol hydrochloride (1:1)
Phenol, 4-[(1E)-1-[4-[2-(methylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]-, hydrochloride (1:1)
Endoxifen
E-isomer hydrochloride
Endoxifen (E-isomer hydrochloride)
Top Suppliers:I want be here




Get all suppliers and price by the below link:

Endoxifen (E-isomer hydrochloride) suppliers


Price: $396/10mM*1mLinDMSO

Reference only. check more Endoxifen (E-isomer hydrochloride) price