I. Basic Information

• Product Name: Toremifene Citrate

• CAS Number: 89778-27-8

• Molecular Formula: C32H36ClNO8 (also reported as C26H28ClNO·C6H8O7)

• Molecular Weight: 598.083

II. Physical Properties

• Appearance: White or nearly white powder

• Melting Point: 158164°C (also reported as 160162°C)

• Boiling Point: 535.1°C at 760 mmHg

• Density: 1.045 g/cm³

• Refractive Index: 1.416~1.418

• Flash Point: 277.4°C

• Solubility: Soluble in dimethyl sulfoxide (DMSO) with a solubility greater than 10 mg/mL

III. Chemical Properties

• Category: Second-generation selective estrogen receptor modulator (SERM)

• Mechanism of Action: Binds to estrogen receptors, producing estrogen-like or anti-estrogen effects, or both, depending on the duration of treatment, species, gender, and target organ.

• Biological Activity: IC50 for estrogen receptors is 1 μM. It also effectively inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 values of 0.07 μM and 2.6 μM, respectively.

IV. Uses and Effects

• Primary Use: As an antineoplastic drug, primarily used to treat metastatic breast cancer in postmenopausal women with estrogen receptor-positive or unknown status.

• Pharmacological Effects: Toremifene citrate competes with estrogen for binding to estrogen receptors in breast cancer cell cytoplasm, blocking estrogen-induced DNA synthesis and proliferation of cancer cells. Additionally, some experimental tumors treated with high doses of toremifene citrate have shown non-estrogen-dependent antitumor effects.