Name: GDC-0068 (RG7440)
Price: 260.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    GDC-0068 (RG7440) is a highly selective small molecule inhibitor of Akt with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3. The PI3K-AKT pathway regulates cell growth, survival and tumorigenesis. GDC-0068 binds to and blocks the activation of AKT, which result in cell cycle arrest, inhibition of tumor cell proliferation and induction of tumor cell death. PI3K-AKT is pathway frequently activated in tumors, thus tumors with PTEN or PI3K mutations, which lead to activation of AKT are with high sensitivity to GDC-0068. GDC-0068 is now used for the treatment of human cancers.
    
    1. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. JF Blake, R Xu, JR Bencsik, D Xiao… - Journal of medicinal 2012
    2. Lin J, Sampath D, Nannini MA, et al: Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Canc Res 2013, 19:1760–1772.
- Properties
  - Alternative Name
    
    GDC0068,RG7440,CS0975; (2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-3-(propan-2-ylamino)propan-1-one
    
    CAS Number
    
    1001264-89-6
    
    Molecular Formula
    
    C24H32ClN5O2
    
    Molecular Weight
    
    458
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥22.9 mg/mL in DMSO; insoluble in H2O; ≥28.35 mg/mL in EtOH
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only
- Reference
  - 1. Xin Zhou, Yanghao Zhong, et al. "Location-specific inhibition of Akt reveals regulation of mTORC1 activity in the nucleus." Nat Commun. 2020 Nov 30;11(1):6088. PMID:33257668