ASP-9521
ASP-9521 Basic information
- Product Name:
- ASP-9521
- Synonyms:
-
- ASP-9521
- 1-[1-[(5-Methoxy-1H-indol-2-yl)carbonyl]piperidin-4-yl]-2-methylpropan-2-ol
- AKR1C3 inhibitor
- ASP-9521; ASP 9521; AKR1C3 INHIBITOR; 17??HSD5 INHIBITOR
- [4-(2-Hydroxy-2-methylpropyl)-1-piperidinyl](5-methoxy-1H-indol-2-yl)methanone
- 17HSD5 inhibitor
- ASP 9521. AKR1C3 inhibitor
- ASP9521; ASP-9521; ASP 9521. AKR1C3 INHIBITOR ; 17HSD5 INHIBITOR
- CAS:
- 1126084-37-4
- MF:
- C19H26N2O3
- MW:
- 330.42
- Mol File:
- 1126084-37-4.mol
ASP-9521 Chemical Properties
- 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
ASP-9521 Usage And Synthesis
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
ASP-9521Supplier
- Tel
- sales@boylechem.com
- Tel
- 021-58955995
- sales@medchemexpress.cn
- Tel
- 025-846993838003-8003 18013301590
- njduly@126.com
- Tel
- +1 (866) 930-6790
- info@adooq.com
- Tel
- 13621943973
- sales@shjiyipharmatech.com