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|---|---|---|---|---|---|---|---|
| {[ item.pr_size ]} | {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} | 现货 | 1周 咨询 | - + | 
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| 产品名称 | Androgen Receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Cyproterone acetate | ++++ Androgen Receptor, IC50: 7.1 nM | 98% | |||||||||||||||||
| Apalutamide | +++ Androgen Receptor, IC50: 16 nM | 98% | |||||||||||||||||
| AZD3514 | + Androgen Receptor, Ki: 2.2 μM | 99% | |||||||||||||||||
| Darolutamide | ++++ Androgen receptor, Ki: 11 nM | 98% | |||||||||||||||||
| Flutamide | +++ Androgen Receptor, Ki: 55 nM | 98% | |||||||||||||||||
| Galeterone | ++ Androgen Receptor, IC50: 384 nM | 98% | |||||||||||||||||
| Enzalutamide | +++ Androgen Receptor, IC50: 36 nM | 98% | |||||||||||||||||
| Megestrol | ✔ | 98% | |||||||||||||||||
| Spironolactone | ++ Androgen Receptor, IC50: 77 nM | 98+% | |||||||||||||||||
| Bicalutamide | ++ Androgen Receptor, IC50: 0.16 μM | 99% | |||||||||||||||||
| EPI-001 | + Androgen Receptor, IC50: ~6 μM | 98% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 | 
 | 
| 描述 | The androgen receptor (AR) and the androgen-AR signaling pathway play a significant role in male sexual differentiation and the development and function of male reproductive and non-reproductive organs [7]. Bicalutamide is an AR antagonist with IC50 of 0.16 μM in LNCaP/AR(cs) cell lines. In the setting of Castration-resistant prostate cancer (CRPC), bicalutamide undergoes an antagonist-to-agonist switch, stimulating AR activity and prostate tumor cell growth. In addition, bicalutamide stimulate proliferation of VCaP cells in a dose-dependent manner. The therapeutic effect of bicalutamide (10 mg/kg/d) was conducted in castrate mice bearing LNCaP/AR(cs) xenograft tumors, the antitumor activity of bicalutamide in this model was largely restricted to growth inhibition rather than tumor shrinkage [8]. Notably, Single administration of bicalutamide reduced tumor growth by 79% at defined submaximal doses [9]. | 
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 | 
| CHO-K1 cells | Function assay | 2 h | Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting, IC50=0.2 μM | 20381361 | |
| COS1 cells | Function assay | Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as reduction in receptor-mediated transcriptional activity by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay, IC50=0.0869 μM | 25646649 | ||
| COS7 cells | Function assay | Agonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay, EC50=0.18 μM | 22094279 | ||
| CV1 cells | Function assay | Binding affinity to human androgen receptor expressed in CV1 cells, Ki=0.151 μM | 17257838 | ||
| Dose | Rat: 10 mg/kg, 20 mg/kg[3] (p.o.); 1 mg/kg - 250 mg/kg[4] (p.o.) Nude mice: 150 mg/kg[5] (p.o.), 50 mg/kg - 100 mg/kg[6] (p.o.) Dog: 0.1 mg/kg - 100 mg/kg[4] (p.o.); 0.25 mg/kg, 2.5 mg/kg[4] (i.v.) | ||||||||||||||||||||||||||||||
| Administration | p.o. | ||||||||||||||||||||||||||||||
| Pharmacokinetics | 
 | 
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 | 
| NCT00298155 | Cancer Prosta... 展开 >>te Neoplasms 收起 << | Phase 2 | Completed | - | United States, Washington ... 展开 >> Veterans' Administration Puget Sound Health Care System (VAPSHCS) Seattle, Washington, United States, 98108-1532 University of Washington Seattle, Washington, United States, 98195-6158 收起 << | 
| NCT00298155 | - | Completed | - | - | |
| NCT02064036 | Adenocarcinoma of the Prostate | Not Applicable | Recruiting | October 2018 | United States, California ... 展开 >> UC Davis Sacramento Cancer Center Dept of Radiation Oncology Recruiting Sacramento, California, United States, 95817 Contact: Richard Valicenti, MD 916-724-8295 rkvalicenti@ucdavis.edu Principal Investigator: Richard Valicenti, MD 收起 << | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 2.32mL 0.46mL 0.23mL | 11.62mL 2.32mL 1.16mL | 23.24mL 4.65mL 2.32mL | |
| CAS号 | 90357-06-5 | 
| 分子式 | C18H14F4N2O4S | 
| 分子量 | 430.37 | 
| SMILES Code | O=C(NC1=CC=C(C#N)C(C(F)(F)F)=C1)C(C)(O)CS(=O)(C2=CC=C(F)C=C2)=O | 
| MDL No. | MFCD00869971 | 
| 别名 | 毕卡鲁胺 ;ICI 176334; ZD 176334; Abbreviation | 
| 运输 | 蓝冰 | 
| InChI Key | LKJPYSCBVHEWIU-UHFFFAOYSA-N | 
| Pubchem ID | 2375 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C | 
| 溶解方案 | DMSO: 50 mg/mL(116.18 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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 
 
 
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