Catalog No.S7827 Synonyms: Afimoxifene
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.
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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.
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|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.|
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. 4-HT activates on-target modification frequency for intein-Cas9 variants .
|In vitro||DMSO||77 mg/mL (198.7 mM)|
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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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