ASP-9521
产品说明书
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同义名 : | - |
| CAS号 : | 1126084-37-4 | |
| 货号 : | A983598 | |
| 分子式 : | C19H26N2O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 330.42 | |
| MDL号 : | MFCD30532740 | |
| 存储条件： |
Pure form Inert atmosphere, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | ASP9521 is a potent, selective, orally bioavailable AKR1C3 inhibitor. ASP9521 inhibited conversion of androstenedione (AD) into testosterone (T) by recombinant human or cynomolgus monkey AKR1C3 in a concentration-dependent manner (IC50, human: 11 nM; IC50, monkey: 49 nM). In LNCaP-AKR1C3 cells, ASP9521 suppressed AD-dependent PSA production and cell proliferation. In CWR22R xenografts, single oral administration of ASP9521 (3 mg/kg) inhibited AD-induced intratumoural T production and this inhibitory effect was maintained for 24 h. After oral administration, ASP9521 was rapidly eliminated from plasma, while its intratumoural concentration remained high. The bioavailability of ASP9521 after oral administration (1 mg/kg) was 35 %, 78 % and 58 % in rats, dogs and monkeys, respectively[1]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01352208 | Castrate Resistant Prostate Ca... 展开 >>ncer 收起 << | Phase 1 Phase 2 | Terminated(It was decided to d... 展开 >>iscontinue the development in consideration of the results of a P1 study) 收起 << | - | Belgium ... 展开 >> Site 131 Antwerp, Belgium, 2650 France Site: 121 Villejuif, France United Kingdom Site:109 Glasgow, United Kingdom Site: 101 Surrey, United Kingdom 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.03mL 0.61mL 0.30mL |
15.13mL 3.03mL 1.51mL |
30.26mL 6.05mL 3.03mL |
| 参考文献 |
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