Imlunestrant

Boiling point: 682.9±55.0°C

Storage temp: -20℃

Solubility: DMSO: 250 mg/mL (476.64 mM; Need ultrasonic)

Form: Solid

Color: Light Yellow to Yellow

Cell Experiment

Solubility in DMSO: 175 mg/mL (333.64 mM; sonication-assisted dissolution; hygroscopic DMSO significantly affects product solubility, so use freshly opened DMSO.)

Preparing Stock Solutions：

Please prepare the stock solution in the appropriate solvent based on the product's solubility in different solvents. Once prepared, aliquot and store to avoid freeze-thaw cycles that may cause product loss.

Stock solution storage and expiration date: -80℃, 6 months; -20℃, 1 month. When stored at -80℃, use within 6 months; when stored at -20℃, use within 1 month.

Imlunestrant is an estrogen receptor (ER) antagonist that induces degradation of ERα, leading to inhibition of ER-dependent gene transcription and cellular proliferation in ER+ breast cancer cells. Imlunestrant demonstrated in vitro and in vivo antitumour activity in ER+ breast cancer xenograft models, including models with ESR1 mutations. Imlunestrant exposure-response relationships and the time course of pharmacodynamics have not been fully characterized.

Estrogen receptor signalling has closely been tied to breast cancer progression and cancer cell proliferation. Estrogen receptor alpha (ERα) has been primarily implicated in breast cancer, and its activation promotes the expression of oncogenic factors that increase cancer cell proliferation, such as MYC, Cyclin D1, FOXM1, GREB1, BCL2 or amphiregulin, IGF-1 and CXCL12. Imlunestrant binds to ERα with high affinity and, in vitro, induces degradation of ERα: This leads to the inhibition of ER-dependent gene transcription and cellular proliferation in ER+ breast cancer cells.