SAR439859

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SAR439859 是一种口服活性非甾体类雌激素受体 (SERD) 选择性降解剂。

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).

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Animal Model:Nu/nu mouse with MCF7 tumor xenograft model Dosage:2.5, 5, 12.5, 25 mg/kg Administration:Orally; twice daily for 30 days Result:Exhibited substantial tumor-growth inhibition and displayed tumor regression at the dose of 25 mg/kg/BID.Animal Model:Mouse, rat and dog Dosage:3 mg/kg (iv) and 10 mg/kg (po) (Pharmacokinetic Analysis) Administration:Iv or po Result:Showed a low to moderate clearance in the three animal species tested (0.03-1.92 L/h?kg), low to moderate volume of distribution (Vss=0.5-6.1 L/kg), and good bioavailability (54-76%) across species.

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Endocrinology/Hormones

Estrogen Receptor/ERR

ERα

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2114339-57-8

554.48

C31H30Cl2FNO3

>98% (HPLC)

DMSO:125 mg/mL?(225.44 mM;?Need ultrasonic)

C1CC2=C(C=CC(=C2)C(=O)O)C(=C(C1)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)O[C@H]5CCN(C5)CCCF

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(-20℃)

With Ice Pack

≥ 2 years