SAR439859 是一种有效的 ER 拮抗剂，具有 ER 降解活性，EC50为 0.2 nM。它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)。它可在 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。

SAR439859 is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD). SAR439859 is a potent antagonist of ER (with an EC50 of 0.2 nM for ERα degradation).

in vivo SAR439859 induces strong antitumor activity against a variety of BC cell lines and patient-derived xenografts, including models that harbor ERα mutations[1].

SAR439859(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[1]. It is noticed that T1/2 was variable across species (1.98 h in mouse, 4.13 h in rat and 9.80 h in dog)[1].

2114339-57-8

C31H30Cl2FNO3

554.48

SAR439859

DMSO:125 mg/mL (225.44 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years