Categories
- PROTAC Linker
- Protein Control Ligand
- Pathway Inhibitors
- Function Modulators
- Activators
- G Protein-Coupled Receptor Ligands
- Nuclear Receptor Ligands
- GDNF Receptors
- TNF Receptors
- Transcription Factors
- Chemokines
- Cytokine Receptors
- Biomarkers and Buffer Solutions
- Molecular Probes
- Stem Cell Research
- Alzheimer's Disease
- Apoptosis
- Cancer Research
- Epigenetics
- Metabolites
- PET/SPECT Imaging Precursors
- Customized Screening Library
- Ultra Pure Pharmacological Standard
- Tissue Microarray (TMA)
- Proteins and Antibodies
- Primary Cells
- ELISA KIT
- Natural Products
- Lab Equipments
- Humanized Mice for PDX Platform
- Rare Chemicals
- Custom Synthesis
- Antibacterial
- Antifungal
- Antioxidant
- Antiviral
- Molecular Glues
- SARS-CoV
Quantity Discount Table - Order More To Get More Price Discount
| Quantity | mg | Unit Price ($/mg or $/Unit) | Final Price |
|---|---|---|---|
| 1 | 5 | $12.75 | Total: $63.75 |
| 1 | 10 | $10.80 | Total: $108.00 |
| 1 | 25 | $9.15 | Total: $228.75 |
| 1 | 50 | $7.80 | Total: $390.00 |
| 1 | 100 | $6.75 | Total: $675.00 |
Overview
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.
Chemical Properties
| Molecular Formula | C19H26N2O3 |
| Molecular Weight | 330.42 |
| CAS Numbers | 1126084-37-4 |
| Solubility | DMSO |
| Purity | 98% by HPLC |
Storage and Handling
0°C (short term), -20°C (long term), desiccated