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ASP-9521
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ASP-9521图片
CAS NO:1126084-37-4
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
ASP9521
产品介绍
ASP9521是一种选择性,有效,有口服活性的AKR1C3抑制剂。它对人类AKR1C3的IC50值为11 nM。

产品描述

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

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.

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.

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.

Cas No.

1126084-37-4

分子式

C19H26N2O3

分子量

330.32

别名

ASP9521

储存和溶解度

DMSO:300 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years