Amcenestrant,2114339-57-8

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Amcenestrant

CAS No. : 2114339-57-8

MCE 国际站：Amcenestrant

产品活性：SAR439859 (compound 43d) 是一种具有口服活性，非甾体和选择性雌激素受体降解剂 (SERD)。SAR439859 是一种有效的 ER 拮抗剂，具有 ER 降解活性，EC₅₀ 为 0.2 nM。SAR439859 可在 ER⁺ 乳腺癌中表现出强大的抗肿瘤功效和有限的交叉耐药性。

研究领域：Vitamin D Related/Nuclear Receptor

作用靶点：Estrogen Receptor/ERR

In Vitro: SAR439859 (compound 43d) induces strong in vivo antitumor activity against a variety of BC cell lines and patient-derived xenografts, including models that harbor ERα mutations.

In Vivo: SAR439859 (compound 43d; orally; 2.5-25 mg/kg; twice daily for 30 days) exhibits substantial tumor-growth inhibition and displays tumor regression at the dose of 25 mg/kg/BID.
?SAR439859 (3 mg/kg for iv and 10 mg/kg for po) shows a low to moderate clearance in the three animal species tested (0.03-1.92 L/h?kg), low to moderate volume of distribution (V_ss=0.5-6.1 L/kg), and good bioavailability (54-76%) across species. It is noticed that T_1/2 was variable across species (1.98 h in mouse, 4.13 h in rat and 9.80 h in dog).

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