Endoxifen HCl

Catalog No.S7839 Batch:S783901

Print

Technical Data

Formula

C25H28ClNO2
Molecular Weight 409.95 CAS No. 1032008-74-4
Solubility (25°C)* In vitro DMSO 74 mg/mL (180.5 mM)
Ethanol 74 mg/mL (180.5 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% corn oil
0.3mg/ml Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 20% PEG 300 5%Tween80 70% water
2.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 200 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue adding Adjust the volume to 1 mL with 700 μL ddH2O. The mixed solution should be used immediately for optimal results. 
* <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.

Selleck's Endoxifen HCl has been cited by 6 publications

Antiviral Activity of Selective Estrogen Receptor Modulators against Severe Fever with Thrombocytopenia Syndrome Virus In Vitro and In Vivo [ Viruses, 2024, 16(8)1332] PubMed: 39205306
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

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.