Endoxifen HCl
Catalog No.S7839
Molecular Weight(MW): 409.95
Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
Cited by 1 publication
Purity & Quality Control
Choose Selective Estrogen/progestogen Receptor Inhibitors
Biological Activity
| Description | Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2. | |||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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
| Cell Research:[2] |
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| Animal Research:[3] |
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Solubility (25°C)
| In vitro | DMSO | 74 mg/mL (180.5 mM) |
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| Ethanol | 74 mg/mL (180.5 mM) | |
| Water | 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.
Chemical Information
| Molecular Weight | 409.95 |
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| Formula | C25H28ClNO2 |
| CAS No. | 1032008-74-4 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| NCT03582865 | Not yet recruiting | Drug: Tamoxifen 20 mg | Breast Cancer | Assiut University | September 1 2019 | -- |
| NCT03504631 | Recruiting | Other: No intervention | Breast Cancer Female | Trisakti University|Dharmais National Cancer Center Hospital | October 1 2017 | -- |
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