4-Hydroxytamoxifen(Afimoxifene)
For research use only. Not for use in humans.
Catalog No.S7827 Synonyms: Afimoxifene
5 publications
Molecular Weight(MW): 387.51
4-Hydroxytamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants.
Selleck's 4-Hydroxytamoxifen(Afimoxifene) has been cited by 5 publications
1 Customer Review
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CDK4/6 inhibitor resistance promotes diminished ER expression and activity. (a and b) Proliferation of MCF-7 and MR cells in the presence of different concentrations of ICI (a) or 4-hydroxytamoxifen (4-OHT) (b) was measured by the alamarBlue assay and plotted as % inhibition of proliferation against log concentration of inhibitor. Each data point represents the average value±s.d. of six replicates obtained in three independent experiments.
Oncogene, 2016, 36(16):2255-2264. 4-Hydroxytamoxifen(Afimoxifene) purchased from Selleck.
Purity & Quality Control
Choose Selective Estrogen/progestogen Receptor Inhibitors
Biological Activity
| Description | 4-Hydroxytamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
4-OHT is a potent activator of ER and has been shown to have a higher affinity for estrogen receptors compared to tamoxifen. It has significant dose and time-dependent direct effects to alter the contractile function of isolated adult rat cardiac myocytes[1]. 4-HT activates on-target modification frequency for intein-Cas9 variants [3]. |
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| Cell Data |
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Protocol
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Solubility (25°C)
| In vitro | DMSO | 77 mg/mL (198.7 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | 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 | 387.51 |
|---|---|
| Formula | C26H29NO2 |
| CAS No. | 68392-35-8 |
| Storage | powder |
| in solvent | |
| Synonyms | Afimoxifene |
| Smiles | CCC(C1=CC=CC=C1)=C(C2=CC=C(O)C=C2)C3=CC=C(OCCN(C)C)C=C3 |
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Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT03199963 | Terminated | Drug: 4-OH tamoxifen|Drug: Placebo | Mammographic Breast Density | BHR Pharma LLC | August 21 2017 | Phase 3 |
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