Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rintodestrant (G1T48) is an orally active, non-steroidal, selective estrogen receptor degrader (SERD) that also functions as a CDK4/6 inhibitor.
Description | Rintodestrant (G1T48) is an orally active, non-steroidal, selective estrogen receptor degrader (SERD) that also functions as a CDK4/6 inhibitor. |
In vitro | Rintodestrant (G1T48) serves as a potent and effective inhibitor, targeting estrogen-mediated transcription and proliferation specifically in ER-positive breast cancer cells, mirroring the efficacy of the pure antiestrogen agent fulvestrant. Its activity is exclusive to ER-positive breast cancer cells, showing no effect on ER-negative cell types. In a Cell Viability Assay utilizing MCF7 cells at concentrations ranging from 1 pM to 1 μM over an incubation period of 18 hours, Rintodestrant demonstrated a significant downregulation of the estrogen receptor, markedly inhibiting estrogen-stimulated growth in these cells with a potency approximately threefold greater than that of Fulvestrant. Notably, this inhibition does not influence apoptosis within MCF7 breast cancer cells. |
In vivo | Rintodestrant (G1T48, 30 or 100 mg/kg) effectively suppresses estrogen signaling in models of endocrine-resistant breast cancer, specifically in MCF7 xenograft tumors[1]. Administered orally at doses of 30 or 100 mg/kg daily for a duration of 28 days, it exhibits a dose-dependent reduction in TamR tumor growth. |
Synonyms | G1T48 |
Molecular Weight | 462.49 |
Formula | C26H19FO5S |
CAS No. | 2088518-51-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Rintodestrant 2088518-51-6 G1T48 inhibitor inhibit