Endoxifen (E-isomer)|SERM|cas 1197194-61-8|DC Chemicals

Cas No.:	1197194-61-8
Chemical Name:	Endoxifen E-isomer hydrochloride
Synonyms:	Endoxifen (E-isomer hydrochloride);E-Endoxifen hydrochloride;Endoxifen E-isomer hydrochloride;Endoxifen (E-isomer);AOB5063;BCP18472;A16343;Phenol, 4-[(1E)-1-[4-[2-(methylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]-, hydrochloride (1:1)
SMILES:	Cl[H].O(C([H])([H])C([H])([H])N([H])C([H])([H])[H])C1C([H])=C([H])C(=C([H])C=1[H])/C(/C1C([H])=C([H])C(=C([H])C=1[H])O[H])=C(/C1C([H])=C([H])C([H])=C([H])C=1[H])\C([H])([H])C([H])([H])[H]
Formula:	C₂₅H₂₈ClNO₂
M.Wt:	409.9483
Purity:	>98%
Sotrage:	4°C for 1 year, -20°C for more than 2 years

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]

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.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC46877	Y134	Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM).
DC42456	Camizestrant ( AZD-9833)	Camizestrant (AZD-9833) is a potent and orally active estrogen receptor (ER) antagonist. Camizestrant is used for the study of ER+ HER2-advanced breast cancer.
DC26134	PROTAC ERRα ligand 2	PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM)[1].
DC7735	XCT790	XCT-790 is a potent, selective and inverse agonist of estrogen-related receptor alpha(ERRα); induces cell death in chemotherapeutic resistant cancer cells.
DC10077	WAY-200070	WAY-200070 is a potent, selective estrogen receptor-beta (ER-β) agonist (IC50 2.3 nM vs 155 nM for ER-α) with anxiolytic-like and antidepressant-like effects.
DC10846	PHTPP	PHTPP is a pyrazolo[1,5-α]pyrimidine-based ligand that acts as a full antagonist of estrogen ERβ receptors with 36-fold selectivity over ERα.
DC10755	LSZ-102	LSZ102 is a potent, orally bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
DCAPI1501	Lasofoxifene tartrate	Lasofoxifene Tartrate is a non-steroidal selective estrogen receptor modulator (SERM).
DC8265	Endoxifen	Endoxifen is a Estrogen receptor α (ERα) ligand; potent antiestrogen,an active metabolite of the cancer drug tamoxifen.
DC9959	Endoxifen (E-isomer)	Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).