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Medchemexpress LLC Asp-9521 | 1126084-37-4 | 98.0% | 330.42 | 50 MG
Supplier: Medchemexpress LLC HY1990350MG
ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.
- IC50: 11 nM (human AKR1C3), 49 nM (monkey AKR1C3)
- Inhibits conversion of androstenedione (AD) into androstenediol and testosterone (T) by recombinant human or cynomolgus AKR1C3.
- Shows more than 100-fold selectivity for AKR1C3 over the isoform AKR1C2.
- Suppresses AD-dependent PSA production and cell proliferation in LNCaP-AKR1C3 cells.
- Single oral administration (3 mg/kg) inhibits AD-induced intratumoural T production in CWR22R xenografts, with the inhibitory effect maintained for 24 h.
- Rapidly eliminated from plasma after oral administration, while intratumoural concentration remained high.
- Bioavailability after oral administration (1 mg/kg) is 35% in rats, 78% in dogs, and 58% in monkeys.
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