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Endoxifen hydrochloride

Catalog No. T6827L CAS 1197194-41-4

Endoxifen hydrochloride, a principal active metabolite of Tamoxifen (TAM), exhibits heightened affinity and specificity towards the estrogen receptor and possesses aromatase inhibitory capability. It holds promise for breast cancer research.

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Endoxifen hydrochloride Chemical Structure

Endoxifen hydrochloride, CAS 1197194-41-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 41.00
10 mg	In stock	$ 66.00
25 mg	In stock	$ 133.00
50 mg	In stock	$ 232.00
100 mg	In stock	$ 374.00
1 mL * 10 mM (in DMSO)	In stock	$ 45.00

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Purity: 99.08%

Biological Description

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Storage & Solubility Information

Description	Endoxifen hydrochloride, a principal active metabolite of Tamoxifen (TAM), exhibits heightened affinity and specificity towards the estrogen receptor and possesses aromatase inhibitory capability. It holds promise for breast cancer research.
In vitro	Endoxifen, an hydroxylated metabolite of Tamoxifen, exhibits approximately 100-fold greater potency as an estrogen receptor (ER) antagonist compared to tamoxifen. Furthermore, it indicates that endoxifen, unlike 4-hydroxytamoxifen, induces degradation of ER-alpha in breast cancer cells in addition to its transcriptional effects on the ER.[1] Endoxifen acts as a potent antiestrogen that promotes the degradation of estrogen receptor α in breast cancer cells. Additionally, it has been demonstrated that endoxifen hinders ERA transcriptional activity and effectively suppresses estrogen-induced proliferation of breast cancer cells, even in the presence of tamoxifen, N-desmethyl-tamoxifen, and 4-hydroxytamoxifen.[2] Endoxifen exhibits significant growth inhibition at a concentration of 10 μM for all breast cancer cell lines, except for MDAMB-468, which shows moderate inhibition. At a concentration of 10 μM, cytotoxic effects are particularly prominent in MCF7, HS 578T, and BT-549 cells. In contrast, lower concentrations of Endoxifen (0.01-1 μM) result in less significant inhibitory effects compared to 10 μM. However, a concentration of 100 μM of Endoxifen is found to be lethal for all tested cells.[2]
In vivo	Endoxifen, when administered orally, is quickly absorbed and readily enters systemic circulation. Administering oral Endoxifen once daily for 28 consecutive days, at dosages of 2, 4, and 8 mg/kg, has demonstrated safety and progressive inhibition of human mammary tumor xenograft growth in female mice.[2]

Molecular Weight	409.95
Formula	C25H28ClNO2
CAS No.	1197194-41-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 0.9 mg/mL (2.2 mM), Sonication and heating to 80℃ are recommended.

DMSO: 31.5 mg/mL (76.8 mM)

References and Literature

1. Goetz MP. Tamoxifen, endoxifen, and CYP2D6: the rules for evaluating a predictive factor. Oncology (Williston Park). 2009;23(14):1233-1236. 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;69(5):1722-1727. 3. Gingery A, et al. The effects of a novel hormonal breast cancer therapy, endoxifen, on the mouse skeleton. PLoS One. 2014;9(5):e98219.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Compound Library Nuclear Receptor Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Endoxifen hydrochloride 1197194-41-4 Endoxifenhydrochloride Endoxifen Hydrochloride inhibitor inhibit

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