4-Hydroxytamoxifen (Afimoxifene)

Catalog No.S7827 Batch:S782702

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Technical Data

Formula

C26H29NO2
Molecular Weight 387.51 CAS No. 68392-35-8
Solubility (25°C)* In vitro DMSO 77 mg/mL (198.7 mM)
Water Insoluble
Ethanol 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.)

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Biological Activity

Description 4-Hydroxytamoxifen (Afimoxifene) 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.
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].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Adult Rat and Mouse Cardiac Myocytes

  • Concentrations

    0, 0.5, 1, 3, 5, and 10 µM

  • Incubation Time

    15-45 min

  • Method

    For sarcomere length measurements, cells are covered in Tyrode’s containing 4OHT, allowed to reach 36 ± 1°C, and then stimulated at 0.2 Hz.
Animal Study:

[2]
  • Animal Models

    Sprague-Dawley rats

  • Dosages

    21 mg/kg, 54 μmol/kg

  • Administration

    oral administration

Customer Product Validation

, , Oncogene, 2016, 36(16):2255-2264

Selleck's 4-Hydroxytamoxifen (Afimoxifene) has been cited by 27 publications

Histone lysine demethylase 4 family proteins maintain the transcriptional program and adrenergic cellular state of MYCN-amplified neuroblastoma [ Cell Rep Med, 2024, 5(3):101468] PubMed: 38508144
The ARID1A-METTL3-m6A axis ensures effective RNase H1-mediated resolution of R-loops and genome stability [ Cell Rep, 2024, 43(2):113779] PubMed: 38358891
Macrophages Promote Subtype Conversion and Endocrine Resistance in Breast Cancer [ Cancers (Basel), 2024, 16(3)678] PubMed: 38339428
Novel Estrogen Receptor Dimerization BRET-Based Biosensors for Screening Estrogenic Endocrine-Disrupting Chemicals [ Biomater Res, 2024, 28:0010] PubMed: 38464469
Single cell multiomic analysis reveals diabetes-associated β-cell heterogeneity driven by HNF1A [ Nat Commun, 2023, 14(1):5400] PubMed: 37669939
Single cell multiomic analysis reveals diabetes-associated β-cell heterogeneity driven by HNF1A [ Nat Commun, 2023, 14(1):5400] PubMed: 37669939
AZI2 mediates TBK1 activation at unresolved selective autophagy cargo receptor complexes with implications for CD8 T-cell infiltration in breast cancer [ Autophagy, 2023, 21:1-16.] PubMed: 37733921
Liver X Receptor Inverse Agonist GAC0001E5 Impedes Glutaminolysis and Disrupts Redox Homeostasis in Breast Cancer Cells [ Biomolecules, 2023, 13(2)345] PubMed: 36830714
SRSF5 Regulates the Expression of BQ323636.1 to Modulate Tamoxifen Resistance in ER-Positive Breast Cancer [ Cancers (Basel), 2023, 15(8)2271] PubMed: 37190199
Alternative promoters and splicing create multiple functionally distinct isoforms of oestrogen receptor alpha in breast cancer and healthy tissues [ Cancer Med, 2023, 12(18):18931-18945] PubMed: 37676103

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.