ASP-9521

Research use only, not for human use.

ASP-9521 is an effective, specific and orally available AKR1C3 inhibitor (IC50: 11 nM, for human).

ASP9521 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.

ASP9521;AKR1C3 inhibitor;17HSD5 inhibitor

Others

Other Targets

AKR1C3

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1126084-37-4

330.32

C19H26N2O3

95%

DMSO : ≥ 300 mg/mL 907.94 mM

CC(C)(CC1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)OC)O

(4-(2-hydroxy-2-methylpropyl)piperidin-1-yl)(5-methoxy-1H-indol-2-yl)methanone.

(-20℃)

With Ice Pack

≥ 2 years