An inhibitor of 17β-HSD5/AKR1C3 (IC50 = 120 nM); selective for 17β-HSD5/AKR1C3 over AKR1C2 (IC50 = 20 μM); inhibits conversion of androstenedione into testosterone by 17β-HSD5/AKR1C3 (IC50s = 11 and 49 nM for human and cynomolgus monkey enzymes

ASP9521 – 25 mg

Brand:
Cayman
CAS:
1126084-37-4
Storage:
-20
UN-No:
Non-Hazardous - /

ASP9521 is an inhibitor of 17β-hydroxysteroid dehydrogenase type 5/aldo-keto reductase 1C3 (17β-HSD5/AKR1C3; IC50 = 120 nM).{45212} 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.  

 

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Description

An inhibitor of 17β-HSD5/AKR1C3 (IC50 = 120 nM); selective for 17β-HSD5/AKR1C3 over AKR1C2 (IC50 = 20 μM); inhibits conversion of androstenedione into testosterone by 17β-HSD5/AKR1C3 (IC50s = 11 and 49 nM for human and cynomolgus monkey enzymes, respectively); inhibits androstenedione-dependent PSA production in and proliferation of LNCaP cells expressing 17β-HSD5/AKR1C3; inhibits androstenedione-induced intratumor testosterone production in a CWR22R prostate cancer mouse xenograft model at 3 and 10 mg/kg

Formal name: [4-(2-hydroxy-2-methylpropyl)-1-piperidinyl](5-methoxy-1H-indol-2-yl)-methanone

Synonyms: 

Molecular weight: 330.4

CAS: 1126084-37-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Sterol Biosynthesis||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Androgens

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