ASP-9521

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP20729CAS No. ：1126084-37-4Purity：98%

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CAS No.	1126084-37-4	Cat. No.	BCP20729
Name	ASP-9521
Synonyms	ASP9521; ASP 9521; AKR1C3 inhibitor ; 17HSD5 inhibitor;
SMILES	O=C(N1CCC(CC(C)(O)C)CC1)C(N2)=CC3=C2C=CC(OC)=C3
Chemical Name
Formula	C19H26N2O3	M. Wt	330.42
Purity	98%	Storage	Store at 4-8°C
Description	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.