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Chemical Structure : ASP9521
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; displays >100-fold selectivity for AKR1C3 over the isoform AKR1C2, and does not inhibits AKR1C1 and AKR1C6; inhibits both aandrostenedione (10 nM)-induced PSA production and cell proliferation in LNCaPAKR1C3 cells with IC50 of 11 nM and 6.6 nM, respectively; inhibits AD-induced intratumoural T production in CWR22R xenografts.
Prostate Cancer
Phase 2 Discontinued
| M.Wt | 330.428 | |
| Formula | C19H26N2O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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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