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ASP-9521

ASP-9521
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Purity:96.96%
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ASP-9521

Catalog No. T4529Cas No. 1126084-37-4
ASP-9521 is an effective, specific and orally available AKR1C3 inhibitor (IC50: 11 nM, for human).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
5 mg$39In Stock
10 mg$55In Stock
25 mg$117In Stock
50 mg$195In Stock
100 mg$355In Stock
200 mg$532In Stock
500 mg$815In Stock
1 mL x 10 mM (in DMSO)$43In Stock
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Product Introduction

Bioactivity
Description
ASP-9521 is an effective, specific and orally available AKR1C3 inhibitor (IC50: 11 nM, for human).
In vitro
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.
In vivo
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.
Cell Research
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.
Animal Research
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.
AliasASP9521
Chemical Properties
Molecular Weight330.42
FormulaC19H26N2O3
Cas No.1126084-37-4
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 60 mg/mL (181.59 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.0265 mL15.1323 mL30.2645 mL151.3226 mL
5 mM0.6053 mL3.0265 mL6.0529 mL30.2645 mL
10 mM0.3026 mL1.5132 mL3.0265 mL15.1323 mL
20 mM0.1513 mL0.7566 mL1.5132 mL7.5661 mL
50 mM0.0605 mL0.3026 mL0.6053 mL3.0265 mL
100 mM0.0303 mL0.1513 mL0.3026 mL1.5132 mL

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