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AOB37546
CAS No :1126084-37-4
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Quantity | mg | Unit Price ($/mg or $/Unit) | Final Price |
---|---|---|---|
1 | 100 | $6.75 | Total: $675.00 |
1 | 50 | $7.80 | Total: $390.00 |
1 | 25 | $9.15 | Total: $228.75 |
1 | 10 | $10.80 | Total: $108.00 |
1 | 5 | $12.75 | Total: $63.75 |
Molecular Formula | C19H26N2O3 |
Molecular Weight | 330.42 |
CAS Numbers | 1126084-37-4 |
Storage Condition | 0°C (short term), -20°C (long term), desiccated |
Solubility | DMSO |
Purity | 98% by HPLC |
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.