
ASP-9521
CAS No. 1126084-37-4
ASP-9521( ASP9521 | AKR1C3 inhibitor | 17HSD5 inhibitor )
Catalog No. M17149 CAS No. 1126084-37-4
ASP-9521 is an effective, specific and orally available AKR1C3 inhibitor (IC50: 11 nM, for human).
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
5MG | 35 | In Stock |
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10MG | 50 | In Stock |
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25MG | 105 | In Stock |
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50MG | 176 | In Stock |
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100MG | 320 | In Stock |
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200MG | 479 | In Stock |
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500MG | 734 | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameASP-9521
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NoteResearch use only, not for human use.
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Brief DescriptionASP-9521 is an effective, specific and orally available AKR1C3 inhibitor (IC50: 11 nM, for human).
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DescriptionASP9521 is a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3). ASP9521 has demonstrated anti-tumour activity in in vitro and in vivo preclinical models. ASP9521 inhibited conversion of androstenedione (AD) into testosterone (T) by recombinant human or cynomolgus monkey AKR1C3 in a concentration-dependent manner (IC50,human: 11 nmol/L;?IC50,monkey: 49 nmol/L). ASP9521 showed >100-fold selectivity for AKR1C3 over the isoform AKR1C2. In LNCaP-AKR1C3 cells, ASP9521 suppressed AD-dependent PSA production and cell proliferation. In patients with mCRPC, ASP9521 demonstrated dose-proportional increase in exposure over the doses evaluated, with an acceptable safety and tolerability profile. However, the novel androgen biosynthesis inhibitor showed no relevant evidence of clinical activity.(In Vitro):AKR1C3 is a promising therapeutic target in castrationresistant prostate cancer, as combination of an AKR1C3 inhibitor and a gonadotropin-releasing hormone analogue may lead to complete androgen blockade.ASP-9521 inhibits conversion of androstenedione (AD) into androstenediol and testosterone (T) by recombinant human or cynomolgus monkey AKR1C3 in a concentrationdependent manner (IC50, human: 11 nM; IC50,monkey: 49 nM). ASP-9521 shows more than 100-fold selectivity for AKR1C3 over the isoform AKR1C2. In LNCaP-AKR1C3 cells, ASP-9521 suppresses AD-dependent PSA production and cell proliferation.(In Vivo):In CWR22R xenografts, single oral administration of ASP-9521 (3 mg/kg) inhibits AD-induced intratumoural T production and this inhibitory effect is maintained for 24 h. After oral administration, ASP-9521is rapidly eliminated from plasma, while its intratumoural concentration remained high. The bioavailability of ASP-9521 after oral administration (1 mg/kg) is 35 %, 78 % and 58 % in rats, dogs and monkeys, respectively.
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In VitroAKR1C3 is a promising therapeutic target in castrationresistant prostate cancer, as combination of an AKR1C3 inhibitor and a gonadotropin-releasing hormone analogue may lead to complete androgen blockade.ASP-9521 inhibits conversion of androstenedione (AD) into androstenediol and testosterone (T) by recombinant human or cynomolgus monkey AKR1C3 in a concentrationdependent manner (IC50, human: 11 nM; IC50,monkey: 49 nM). ASP-9521 shows more than 100-fold selectivity for AKR1C3 over the isoform AKR1C2. In LNCaP-AKR1C3 cells, ASP-9521 suppresses AD-dependent PSA production and cell proliferation.
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In VivoIn CWR22R xenografts, single oral administration of ASP-9521 (3 mg/kg) inhibits AD-induced intratumoural T production and this inhibitory effect is maintained for 24 h. After oral administration, ASP-9521is rapidly eliminated from plasma, while its intratumoural concentration remained high. The bioavailability of ASP-9521 after oral administration (1 mg/kg) is 35 %, 78 % and 58 % in rats, dogs and monkeys, respectively.
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SynonymsASP9521 | AKR1C3 inhibitor | 17HSD5 inhibitor
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PathwayOthers
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TargetOther Targets
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RecptorAKR1C3
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Research Area——
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Indication——
Chemical Information
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CAS Number1126084-37-4
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Formula Weight330.32
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Molecular FormulaC19H26N2O3
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 300 mg/mL 907.94 mM
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SMILESCC(C)(CC1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)OC)O
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Chemical Name(4-(2-hydroxy-2-methylpropyl)piperidin-1-yl)(5-methoxy-1H-indol-2-yl)methanone.
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Kikuchi A, et al. .Invest New Drugs. 2014 Oct;32(5):860-70.
molnova catalog



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