Rintodestrant(Synonyms: G1T48)

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Rintodestrant (Synonyms: G1T48)

Rintodestrant (G1T48) 是具有口服活性的、非甾体类的、选择性的雌激素受体 (estrogen receptor) 的降解剂。Rintodestrant (G1T48) 也是 CDK4/6 的抑制剂。

Rintodestrant(Synonyms: G1T48)

Rintodestrant Chemical Structure

CAS No. : 2088518-51-6

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10 mg ￥8500 询问价格 & 货期

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生物活性

Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor[1].

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

Rintodestrant (G1T48, 30 or 100 mg/kg) inhibits estrogen signaling in endocrine-resistant breast cancer models[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

462.49

Formula

C26H19FO5S
CAS 号

2088518-51-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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