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CAS No.: 1126084-37-4

ASP-9521 Catalog No. CSN22691

Synonyms: 17HSD5 inhibitor

ASP 9521 is a potent and selective AKR1C3 inhibitor with IC50 of 11 nM for human AKR1C3.

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实验方案

技术信息

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... more >>ncer Collapse <<	Phase 1 Phase 2	Terminated(It was decided to d... more >>iscontinue the development in consideration of the results of a P1 study) Collapse <<	-	Belgium ... more >> Site 131 Antwerp, Belgium, 2650 France Site: 121 Villejuif, France United Kingdom Site:109 Glasgow, United Kingdom Site: 101 Surrey, United Kingdom Collapse <<

参考文献

[1] Kikuchi A, Furutani T, Azami H, Watanabe K, Niimi T, Kamiyama Y, Kuromitsu S, Baskin-Bey E, Heeringa M, Ouatas T, Enjo K. In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3). Invest New Drugs. 2014 Oct;32(5):860-70

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0264 mL
- 15.1322 mL
- 30.2644 mL
- 5 mM
- 0.6053 mL
- 3.0264 mL
- 6.0529 mL
- 10 mM
- 0.3026 mL
- 1.5132 mL
- 3.0264 mL

技术信息

CAS号

1126084-37-4

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H26N2O3

运输

蓝冰

分子量

330.42

别名

17HSD5 inhibitor

溶解度

DMSO	440.0 mg/mL (1331.6 mM)
Water	insoluble

动物实验配方

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