| Identification | Back Directory | [Name]
ASP-9521 | [CAS]
1126084-37-4 | [Synonyms]
ASP-9521
ASP-9521, >98%
17HSD5 inhibitor
AKR1C3 inhibitor
ASP 9521. AKR1C3 inhibitor
Inhibitor,inhibit,ASP-9521,ASP 9521
ASP-9521; ASP 9521; AKR1C3 INHIBITOR; 17??HSD5 INHIBITOR
ASP9521; ASP-9521; ASP 9521. AKR1C3 INHIBITOR ; 17HSD5 INHIBITOR
1-[1-[(5-Methoxy-1H-indol-2-yl)carbonyl]piperidin-4-yl]-2-methylpropan-2-ol
[4-(2-Hydroxy-2-methylpropyl)-1-piperidinyl](5-methoxy-1H-indol-2-yl)methanone
(4-(2-Hydroxy-2-methylpropyl)piperidin-1-yl)(5-methoxy-1H-indol-2-yl)methanone
Methanone, [4-(2-hydroxy-2-methylpropyl)-1-piperidinyl](5-methoxy-1H-indol-2-yl)- | [Molecular Formula]
C19H26N2O3 | [MDL Number]
MFCD30532740 | [MOL File]
1126084-37-4.mol | [Molecular Weight]
330.421 |
| Chemical Properties | Back Directory | [Boiling point ]
543.9±30.0 °C(Predicted) | [density ]
1.183±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
DMSO:52.26(Max Conc. mg/mL);158.16(Max Conc. mM)
DMF:10.0(Max Conc. mg/mL);30.26(Max Conc. mM)
DMF:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.51(Max Conc. mM)
Ethanol:36.35(Max Conc. mg/mL);110.01(Max Conc. mM) | [form ]
A crystalline solid | [pka]
15.23±0.29(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
ASP9521 is an inhibitor of 17β-hydroxysteroid dehydrogenase type 5/aldo-keto reductase 1C3 (17β-HSD5/AKR1C3; IC50 = 120 nM). It is selective for 17β-HSD5/AKR1C3 over AKR1C2 (IC50 = 20 μM). ASP9521 inhibits conversion of androstenedione into testosterone by 17β-HSD5/AKR1C3 (IC50s = 11 and 49 nM for human and cynomolgus monkey enzymes, respectively). It inhibits androstenedione-dependent production of prostate specific androgen (PSA) in and proliferation of LNCaP cells expressing 17β-HSD5/AKR1C3. ASP9521 (3 and 10 mg/kg) inhibits androstenedione-induced intratumor testosterone production in a CWR22R prostate cancer mouse xenograft model. | [Uses]
ASP 9521 is a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3). AKR1C3 is a promising therapeutic target in castration-resistant prostate cancer | [in vivo]
In CWR22R xenografts, single oral administration of ASP-9521 (3 mg/kg) inhibits AD-induced intratumoural T production and this inhibitory effect is maintained for 24 h. After oral administration, ASP-9521is 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[1]. | [References]
[1] AYA KIKUCHI. In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3).[J]. Investigational New Drugs, 2014, 32 5: 860-870. DOI: 10.1007/s10637-014-0130-5 |
|
|