ASP9521

ASP9521 is an inhibitor of 17beta-hydroxysteroid dehydrogenase type 5/aldo-keto reductase 1C3 (17beta-HSD5/AKR1C3, IC50 = 120 nM). It is selective for 17beta-HSD5/AKR1C3 over AKR1C2 (IC50 = 20 µM). ASP9521 inhibits conversion of androstenedione into testosterone by 17beta-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 17beta-HSD5/AKR1C3. ASP9521 (3 and 10 mg/kg) inhibits androstenedione-induced intratumor testosterone production in a CWR22R prostate cancer mouse xenograft model.Formal Name: [4-(2-hydroxy-2-methylpropyl)-1-piperidinyl](5-methoxy-1H-indol-2-yl)-methanone. CAS Number: 1126084-37-4. Molecular Formula: C19H26N2O3. Formula Weight: 330.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/mL, DMF:PBS (pH 7.2) (1:1): 0.5 mg/mL, DMSO: 10 mg/mL, Ethanol: 10 mg/mL. lambdamax: 214, 294 nm. SMILES: CC(C)(O)CC1CCN(C(C2=CC3=C(C=CC(OC)=C3)N2)=O)CC1. InChi Code: InChI=1S/C19H26N2O3/c1-19(2,23)12-13-6-8-21(9-7-13)18(22)17-11-14-10-15(24-3)4-5-16(14)20-17/h4-5,10-11,13,20,23H,6-9,12H2,1-3H3. InChi Key: OXSCPDKUZWPWFR-UHFFFAOYSA-N.