Active Pharmaceutical Ingredients

Tamoxifen is a nonsteroidal anti estrogen drug. Its structure is similar to estrogen, and there are two isomers, Z-type and E-type. Their physical and chemical properties are different, and their physiological activities are also different. Type E has weak estrogen activity, while type Z has anti estrogen effect. If there is estrogen receptor (ER) in breast cancer cells, estrogen enters the tumor cells and combines with it to promote the synthesis of DNA and mRNA of tumor cells and stimulate the growth of tumor cells. The z-isomer of tamoxifen enters the cell and competes with Er to form receptor complex, which prevents the role of estrogen and thus inhibits the proliferation of breast cancer cells.

Molecular Formula: C26H29NO,C6H8O7

Molecular Weight: 563.6

CAS No.: 54965-24-1

Description

Tamoxifen citrate is the trans-isomer of a triphenylethylene derivative. The pKa’ is 8.85, the equilibrium solubility in water at 37°C is 0.5 mg/mL and in 0.02 N HCl at 37°C, it is 0.2 mg/mL.

Application

It is mainly used in patients with breast cancer with high estrogen level. Combined with androgen and other anti-tumor drugs (such as adriamycin, etc.), it can improve the curative effect, and has a good curative effect on postmenopausal advanced breast cancer.

Packing and Storage

Preserve in well-closed, light-resistant containers.

Minimum Order

One package

Category	Information
Chemical Properties	– Molecular Formula: C₂₆H₂₉NO₂<br>- Molecular Weight: 384.51 g/mol
Physical Properties	– Appearance: White to off-white powder
Mechanism of Action	– Selective estrogen receptor modulator (SERM) that competitively inhibits estrogen binding in breast cells while activating estrogen activity in other tissues such as bones, liver, and uterus.<br>- Acts as an Hsp90 activator, enhancing the ATPase activity of the Hsp90 molecular chaperone.
Biological Activities	– Inhibits cell proliferation in various cancer cell lines, including MCF-7 (IC₅₀ = 0.796 μM), MDA-MB-231 (IC₅₀ = 10.71 μM), and others.<br>- Exhibits antiviral activity against Ebola virus (IC₅₀ = 0.1 μM) and Marburg virus (IC₅₀ = 1.8 μM).<br>- Induces autophagy and apoptosis in cells.
Clinical Uses	– First-generation SERM used for the treatment of breast cancer, ovarian cancer, pancreatic cancer, and malignant melanoma.<br>- Also used as an adjuvant therapy for early and advanced breast cancer.
Safety Information	– Potential side effects include vision changes, retinal lesions, cataracts, and color vision disturbances.<br>- Store at room temperature, protect from light and moisture.
Synonyms	– ICI 46474, Nolvadex, Soltamox

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