An inhibitor of 17β-HSD5/AKR1C3
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ASP9521

Item No. 27308

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mLDMF:PBS (pH 7.2) (1:1): 0.5 mg/mLDMSO: 10 mg/mLEthanol: 10 mg/mL
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

    $102

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    25 mg

    $183

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    Product Description

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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kikuchi, A., Furutani, T., Azami, H., et al. In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3). Invest New Drugs 32(5), 860-870 (2014).