ARN-509

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

ARN-509 是一种选择性、竞争性雄激素受体抑制剂，在无细胞测定中 IC50 为 16 nM，可用于前列腺 Y 治疗。

ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate Y treatment. Phase 3.(In Vitro):Apalutamide (ARN-509) also exhibits low micromolar affinity (IC50 3 μM) for the GABAA receptor in radioligand binding-assays and thus may potentially antagonize GABAA at therapeutic dose levels. Apalutamide is a potent androgen receptor (AR) antagonist that targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets.(In Vivo):Apalutamide (ARN-509) exhibits low systemic clearance, high oral bioavailability and long plasma half-life in both mouse and dog, supporting once-daily oral dosing. Consistent with its long terminal-half-life, Apalutamide steady-state plasma-levels increases in repeat-dose studies, resulting in high C24hr levels and low peak:trough ratios (ratio:2.5). Castrate male mice bearing LNCaP/AR xenograft tumors are treated with either Apalutamide at doses of 1, 10 or 30 mg/kg/day. Thirteen of 20 Apalutamide (30 mg/kg/day)-treated animals exhibit >50% reduction in tumor-volume at day 28 versus 3 of 19 MDV3100 (30 mg/kg/day)-treated mice.

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JNJ-56021927

Endocrinology/Hormones

Androgen Receptor (AR)

Androgen Receptor| GABAR

Cancer

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956104-40-8

477.43

C21H15F4N5O2S

>98% (HPLC)

Ethanol: 5 mg/mL (10.47 mM); DMSO: 18 mg/mL (37.7 mM)

O=C(NC)C1=CC=C(N(C(N(C2=CC(C(F)(F)F)=C(C#N)N=C2)C3=O)=S)C43CCC4)C=C1F

4-(7-(6-cyano-5-(trifluoromethyl)pyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl)-2-fluoro-N-methylbenzamide

(-20℃)

With Ice Pack

≥ 2 years