SAR439859

Research use only, not for human use.

SAR439859 is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD).

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