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ASP9521

Chemical Structure : ASP9521

CAS No.: 1126084-37-4

ASP9521 (ASP 9521;ASP-9521)

Catalog No.: PC-60998Not For Human Use, Lab Use Only.

ASP9521(ASP-9521) is a potent, selective, orally bioavailable inhibitor of Aldo-keto reductase 1C3 (17βHSD5, AKR1C3) with IC50 of 11 nM and 49 nM for recombinant human or cynomolgus monkey AKR1C3, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

ASP9521 (ASP-9521) is a potent, selective, orally bioavailable inhibitor of Aldo-keto reductase 1C3 (17βHSD5, AKR1C3) with IC50 of 11 nM and 49 nM for recombinant human or cynomolgus monkey AKR1C3, respectively.
ASP9521 displays >100-fold selectivity for AKR1C3 over the isoform AKR1C2, and does not inhibits AKR1C1 and AKR1C6.
ASP9521 inhibits both aandrostenedione (10 nM)-induced PSA production and cell proliferation in LNCaPAKR1C3 cells with IC50 of 11 nM and 6.6 nM, respectively.
ASP9521 inhibits AD-induced intratumoural T production in CWR22R xenografts.

Physicochemical Properties

M.Wt 330.428
Formula C19H26N2O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-{1-[(5-methoxy-1H-indol-2-yl)carbonyl]piperidin-4-yl}-2-methylpropan-2-ol

References

1. Loriot Y, et al. Invest New Drugs. 2014 Oct;32(5):995-1004.

2. Kikuchi A, et al. Invest New Drugs. 2014 Oct;32(5):860-70.

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