Endoxifen HCl

Catalog No.S7839 Batch:S783902

Technical Data

Formula	C₂₅H₂₈ClNO₂
Molecular Weight	409.95	CAS No.	1032008-74-4
Solubility (25°C)*	In vitro	DMSO	81 mg/mL (197.58 mM)
		Ethanol	81 mg/mL (197.58 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.

Targets

Estrogen receptor ^[1]

In vitro

Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. ^[1] Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. ^[2] In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. ^[3] Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. ^[4] Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM. ^[5]

In vivo

In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen. ^[3]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines MCF7 and Ishikawa cells Concentrations 1000 nM Incubation Time 8 days Method MCF7 and Ishikawa cells are grown in 10% triple charcoal-stripped serum-containing medium for 3 d. The cells are then plated at a density of 2,000 cells per well in 96-well tissue culture plates and treated as indicated every 48 h. Cell proliferation assays are conducted 8 days after the first treatment using a CellTiter-Glo Luminescent Cell Viability kit according to the manufacturer's protocol.
Animal Study:^{^[3]}	Animal Models Mice bearing MCF-7 human mammary tumor xenografts Dosages 8 mg/kg Administration p.o.

Cell Assay:^{^[2]}

Cell lines
MCF7 and Ishikawa cells
Concentrations
1000 nM
Incubation Time
8 days
Method
MCF7 and Ishikawa cells are grown in 10% triple charcoal-stripped serum-containing medium for 3 d. The cells are then plated at a density of 2,000 cells per well in 96-well tissue culture plates and treated as indicated every 48 h. Cell proliferation assays are conducted 8 days after the first treatment using a CellTiter-Glo Luminescent Cell Viability kit according to the manufacturer's protocol.

Animal Study:^{^[3]}

Animal Models
Mice bearing MCF-7 human mammary tumor xenografts
Dosages
8 mg/kg
Administration
p.o.

References

+ Expand

Selleck's Endoxifen HCl has been cited by 5 publications

Identification of the estrogen receptor beta as a possible new tamoxifen-sensitive target in diffuse large B-cell lymphoma [ Blood Cancer J, 2022, 12(3):36]	PubMed: 35256592
Fatty acid oxidation and autophagy promote endoxifen resistance and counter the effect of AKT inhibition in ER-positive breast cancer cells [ J Mol Cell Biol, 2021, mjab018]	PubMed: 33755174
Targeting Estrogen Receptor-Positive Breast Microtumors with Endoxifen-Conjugated, Hypoxia-Sensitive Polymersomes [ ACS Omega, 2021, 6(42):27654-27667]	PubMed: 34722965
The effect of oestrogen on mandibular condylar cartilage via hypoxia-inducible factor-2α during osteoarthritis development. [ Bone, 2020, 130:115123]	PubMed: 31678498
Estrogen-Related Hormones Induce Apoptosis by Stabilizing Schlafen-12 Protein Turnover. [ Mol Cell, 2019, 75(6):1103-1116.e9]	PubMed: 31420216

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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