Rintodestrant

Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor. In Vitro Rintodestrant (G1T48) is a potent and efficacious inhibitor of estrogen-mediated transcription and proliferation in ER-positive breast cancer cells, similar to the pure antiestrogen fulvestrant. Rintodestrant (G1T48) selectively inhibits the growth of ER-positive, but not ER-negative, breast cancer cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MCF7 cells. Concentration: 1 pM-1 μM. Incubation Time: 18 h. Result: Downregulates the estrogen receptor in breast cancer cells. Significantly inhibited estrogen-mediated growth of MCF7 cells demonstrating approximately threefold higher potency when compared to Fulvestrant. Does not impact apoptosis in MCF7 breast cancer cells. In Vivo Rintodestrant (G1T48, 30 or 100 mg/kg) inhibits estrogen signaling in endocrine-resistant breast cancer models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MCF7 xenograft tumors . Dosage: 30 or 100 mg/kg. Administration: P.O. daily for 28 days. Result: Demonstrated dose-dependent inhibition of TamR tumor growth.

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