首页 Metabolism NADPH ASP9521
ASP9521
编号 T4529     别名: ASP 9521, ASP-9521, ASP-9521 ASP 9521
CAS 1126084-37-4     分子式 C19H26N2O3     分子量 330.32
靶点: AKR1C3;
ASP-9521 is an effective, specific and orally available AKR1C3 inhibitor (IC50: 11 nM, for human).
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规格 库存 单价 数量
2 mg 上海现货 282.00
5 mg 上海现货 507.00
10 mg 上海现货 858.00
25 mg 上海现货 1927.00
50 mg 上海现货 3522.00
100 mg 待询 5900.00
200 mg 待询 9867.00
1 mL * 10 mM (in DMSO) 上海现货 507.00
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生物活性

产品描述

ASP-9521 is an effective, specific and orally available AKR1C3 inhibitor (IC50: 11 nM, for human).

靶点活性

AKR1C3,11nM

体外活性

ASP-9521 concentration-dependently inhibits conversion of androstenedione (AD) into androstenediol and testosterone (T) by recombinant human or cynomolgus monkey AKR1C3 (IC50: 11/49 nM, human/monkey). ASP-9521 has more than 100-fold selectivity for AKR1C3 over the isoform AKR1C2. In LNCaP-AKR1C3 cells, ASP-9521 suppresses AD-dependent PSA production and cell proliferation.

体内活性

In CWR22R xenografts, ASP-9521 (3 mg/kg, p.o.) inhibits AD-induced intratumoural T production and this inhibitory effect is maintained for 24 h. ASP-9521 (p.o.) is rapidly eliminated from plasma, while its intratumoural concentration remained high. The bioavailability of ASP-9521 after oral administration (1 mg/kg) is 35 %, 78 % and 58 % in rats, dogs and monkeys, respectively.

动物实验

ASP-9521 is prepared in 0.5 % methyl cellulose. Mice carrying HEK293 or HEK293-AKR1C3 tumors with similar sizes are selected and randomly divided into 5 groups (N=3 for each group). All groups are treated with ASP-9521 (single oral administration; 3 mg/kg). Plasma (from the central vein) and tumor tissues are collected at 0.25, 0.5, 1, 2 and 4 h after administration of ASP-9521, and ASP-9521 concentrations are determined using the HPLCMS/MS method.

细胞实验

LNCaP-AKR1C3 cells stably expressing human AKR1C3 are seeded in 96-well plates at 10000 cells/100 μL/well in RPMI-1640 medium supplemented with heat-inactivated charcoal-dextran-stripped FBS (1 % for the PSA expression assay and T measurement and 5 % for the cell proliferation assay). After 24 h incubation, AD is added to each well with or without ASP-9521 (0.3-100 nM). The cell culture media are collected 24 h after administration of AD to measure T concentration and 6 days after administration of AD to measure cell proliferation using Cell-Titer Glo assay.

化学信息

分子量

330.32

分子式

C19H26N2O3

CAS

1126084-37-4

溶解度

DMSO: 300 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 3.027 ml 15.137 ml 30.274 ml
5 mM 0.605 ml 3.027 ml 6.055 ml
10 mM 0.303 ml 1.514 ml 3.027 ml
50 mM 0.061 ml 0.303 ml 0.605 ml
相关化合物库
本产品收录于以下化合物库中:
  • 经典已知活性库
  • 抗癌化合物库
  • 抗代谢疾病化合物库
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