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2088518-51-6

2088518-51-6 structure
2088518-51-6 structure
  • Name: Rintodestrant
  • Chemical Name: Rintodestrant
  • CAS Number: 2088518-51-6
  • Molecular Formula: C26H19FO5S
  • Molecular Weight: 462.49
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
  • Create Date: 2022-01-14 16:50:32
  • Modify Date: 2024-04-11 10:54:18
  • Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor[1].

Name Rintodestrant
Description Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor[1].
Related Catalog
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[1]. Rintodestrant (G1T48) selectively inhibits the growth of ER-positive, but not ER-negative, breast cancer cells[1]. Cell Viability Assay[1] Cell 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[1]. Animal Model: MCF7 xenograft tumors[1]. Dosage: 30 or 100 mg/kg. Administration: P.O. daily for 28 days. Result: Demonstrated dose-dependent inhibition of TamR tumor growth.
References

[1]. Kaitlyn J Andreano, et al. G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer. Breast Cancer Res Treat. 2020 Apr;180(3):635-646.

Molecular Formula C26H19FO5S
Molecular Weight 462.49