Chemical Structure : ASP9521
CAS No.: 1126084-37-4
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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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.
M.Wt | 330.428 | |
Formula | C19H26N2O3 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
1-{1-[(5-methoxy-1H-indol-2-yl)carbonyl]piperidin-4-yl}-2-methylpropan-2-ol |
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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