AZD3514 是一种具有口服活性的，选择性的androgen receptor (AR)抑制剂。AZD3514 雄性激素依赖的，以及非依赖的抑制 AR 信号。AZD351 在雄激素缺失的情况下下调 LNCaP 人前列腺癌细胞的核 AR 含量，其pIC50值为 5.75。AZD3514 可用于前列腺癌的研究。
| 生物活性 | AZD3514 is an orally activie and selectiveandrogen receptor(AR)inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostatecancercells in the absence of androgen with anpIC50value of 5.75. AZD3514 can be used for the research of prostatecancer[1][2][3]. |
体外研究
(In Vitro) | AZD3514 (0-10 μM/L; 7 d) inhibits LNCaP and LAPC4 cells proliferation[2].AZD3514 (0-10 μM/L; 24 h) inhibits the ligand-driven expression of known AR-regulated genes[2].AZD3514 (0-30 μM/L; 24 h) reduces AR protein expression in LNCaPs and LAPC4s[2].AZD3514 (1-10 μM/L; 2 h) reduces AR nuclear translocation in LNCaP cells[2].
Cell Proliferation Assay[2] | Cell Line: | LNCaP and LAPC4 cell lines | | Concentration: | 0, 0.1, 0.4, 1.1, 3.3 and 10 μM/L | | Incubation Time: | 7 days | | Result: | Inhibited LAPC4 cells growth and dose-dependently inhibited proliferation of LNCaP cells. |
Western Blot Analysis[2] | Cell Line: | LNCaP and LAPC4 cell lines | | Concentration: | 0, 0.4, 1.1, 3.3, 10 and 30 μM/L | | Incubation Time: | 0-24 hours | | Result: | Dose-dependently reduced AR protein expression in LNCaPs, and decreased AR protein in LAPC4 cells with a concentration of 10 μM/L. Reduced the rate of AR synthesis to reduce the concentration of AR protein. |
RT-PCR[2] | Cell Line: | LNCaP and LAPC4 cell lines | | Concentration: | 0, 0.4, 1.1, 3.3 and 10 μM/L | | Incubation Time: | 24 hours | | Result: | Inhibited ligand-driven expression of AR-regulated genes PSA and TMPRSS2 in both LNCaP and LAPC4 cells. |
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体内研究
(In Vivo) | AZD3514 (10-100 mg/kg; p.o. once daily for 6 days) inhibits AR signaling in rats[2].AZD3514 (50 mg/kg; p.o. once daily for 30 days) inhibits prostate tumor growth[2].AZD3514 (50-100 mg/kg; p.o. once daily for 3 days) significantly reduces nuclear AR protein in vivo[2].
| Animal Model: | Intact or castrat 42- and 49-day-old Hans Wistar rats[2] | | Dosage: | 10, 50 and 100 mg/kg | | Administration: | Oral gavage; 10-100 mg/kg once daily; for 6 days | | Result: | Inhibited AR signaling in rats, reduced seminal vesicle weight in intact rats, and inhibited the ability of exogenous testosterone proprionate to cause an increase in seminal vesicle weight in castrated rat. |
| Animal Model: | Male Copenhagen rats with Dunning R3327H prostate tumors[2] | | Dosage: | 50 mg/kg | | Administration: | Oral gavage; 50 mg/kg once daily; for 30 days | | Result: | Significantly inhibited prostate tumor growth of rats. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(192.47 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.9247 mL | 9.6235 mL | 19.2471 mL | | 5 mM | 0.3849 mL | 1.9247 mL | 3.8494 mL | | 10 mM | 0.1925 mL | 0.9624 mL | 1.9247 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.81 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.81 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.81 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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