Name: GNE-477
Price: 318.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    IC50: 4 and 21 nmol/L for PI3K and mTOR, respectivelyGNE-477 is a potent dual PI3K/mTOR inhibitor. Owing to the common association with oncogenic malignancies, the PI3K/AKT/mTOR signaling pathway is regarded as an attractive area of research for the identification of oral small molecule inhibitors.In vitro: GNE-477 was found to inhibit PI3K-α, β, δ, and γ with IC50s of 4, 86, 6, and 15 nM, respectively. [1]. In vivo: A direct comparison of GNE-477 with its des-methyl analog revealed that the trend of reduced in vivo clearance in rats is also observed in dogs and mice. The clearance improvement was significant in dogs where the des-methyl analog was cleared at two-thirds the rate of hepatic blood flow while GNE-477 had low clearance. In an study evaluating the tumor growth inhibition of a PC3 tumor xenograft10 over 14 days, stasis was achieved at a 20 mg/kg QD dose of GNE-477 and significant inhibition was found with doses as low as 1 mg/kg QD. GNE-477 was generally well tolerated during this study as shown by acceptable levels of weight loss comparable to that in the vehicle cohort [1]. Clinical trial: N/A
- Properties
  - Alternative Name
    
    5-(7-methyl-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine
    
    CAS Number
    
    1032754-81-6
    
    Molecular Formula
    
    C21H28N8O3S2
    
    Molecular Weight
    
    504.63
    
    Purity
    
    98.85%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥16.69 mg/mL in DMSO with gentle warming
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only

GNE-477

GNE-477

Background

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