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抑制剂/激活剂

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凋亡与自噬

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Apalutamide ARN-509

Apalutamide (ARN-509) 是有效，竞争性的雄激素受体 (AR) 拮抗剂，IC50 为 16 nM。

货号：
TK0448
规格：

2mg

10mg

25mg

50mg
价格：
￥0.00

产品参数

CAS No.	956104-40-8
分子式	C21H15F4N5O2S
分子量	477.43
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 50 mg/mL (104.73 mM; Need ultrasonic)
体内研究	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.
体外研究	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.
文献	•Cell Death Dis. 2021 Jul 27;12(8):740. •JCI Insight. 2019 Sep 5;4(17):e122688. •Mol Cancer Ther. 2016 Jul;15(7):1702-12. •Mol Cancer Res. 2017 Jan;15(1):35-44. •Front Pharmacol. 19 July 2021. •Sci Rep. 2019 Sep 24;9(1):13786.
纯度及产品资料	98%

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