Name: ODM-201
Price: 280.00 USD

- Overview
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    Background
    
    ODM-201 is a new-generation inhibitor of androgen receptor with Ki value of 11 nM [1].Androgen receptor is a type of nuclear receptor that is activated by androgen and functions as a DNA-binding transcription factor that regulates gene expression. Activation of androgen receptor (AR) is crucial for prostate cancer growth [1]. ODM-201 is a high-affinity and potent androgen receptor antagonist. In competitive AR binding assays, ODM-201 exhibited Ki value of 11 nM. In AR-HEK293 cells stably expressing full-length human AR (hAR) and an androgen-responsive luciferase reporter gene construct, ODM-201 and its major metabolite ORM-15341 inhibited AR-mediated transactivation with IC50 values of 26 nM and 38 nM. In human U2-OS osteosarcoma cells expressing wtAR or mutant AR(F876L), AR(W741L), or AR(T877A), ODM-201 and ORM-15341 also functioned as full antagonists. in AR overexpressing HS-HEK293 cells, ODM-201 inhibited the androgen-induced nuclear translocation of overexpressed AR. In the VCaP cell line with endogenous AR gene amplification and AR overexpression, ODM-201 inhibited androgen-induced cell proliferation with IC50 value of 230 nM. In castrated male nude mice with subcutaneously injected VCaP cells, orally treatment with ODM-201 (50 mg/kg) once (qd) or twice daily (bid) for 37 days, ODM-201 showed a significant antitumor activity with both doses. There was no sign of treatment-related toxicities. In orthotopic VCaP tumor-bearing intact nude mice, ODM-201 (50 mg/kg, bid) significantly inhibited tumor growth but did not affect the testosterone levels in serum. ODM-201 couldn’t penetrate the blood-brain barrier [1].
- Properties
  - Alternative Name
    
    N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide
    
    CAS Number
    
    1297538-32-9
    
    Molecular Formula
    
    C19H19ClN6O2
    
    Molecular Weight
    
    398.85
    
    Appearance
    
    A solid
    
    Purity
    
    98.02%
    
    Solubility
    
    insoluble in H2O; ≥12.7 mg/mL in EtOH with ultrasonic; ≥19.95 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

ODM-201

ODM-201

Background

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