AZD5363

- Overview
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    Background
    
    AZD5363 is a novel, potent phosphoinositide 3-kinase (PI3K)/Akt pathway inhibitor with IC50 value of ~200nM. [1]
    AZD5363 is proved to inhibit castrate resistant prostate cancer (CRPC) progression. Clusterin (CLU) and autophagy will be induced which may work as cytoprotective responses which can affect the downstream PI3K/Akt signaling. [2] AZD5363 inhibits the growth of a lot of human tumor cells in a dose dependent manner. The mode of action could be monotherapy as well as in combination with HER2 inhibitors in breast cancer models. [3] It is suggested to induce cell apoptosis by measuring the expression of PARP cleavage, the activity of Caspase 3, et al. [1]
    Most importantly, AZD5363 can target the PI3K/Akt-pathway in vivo significantly, thus reducing the serum PSA-levels and tumor volume, finally, it could postpone the progression to CRPC.[1]
    
    [1] Thomas C, Crafter C, Davies B, Zoubeidi A, Gleave ME. AZD5363, A novel AKT inhibitor, delays prostate cancer progression. The Journal of Urology. May 2011. 185(4S): e292-293.
    [2] Kumano M, Zhang F, Shiota M, Crafter C, Davies B, Zoubeidi A, Gleave M. Clusterin knockdown enhances antitumor activity of a novel Akt inhibitor, AZD5363, through inhibition of autophagy in prostate cancer. The Journal of Urology. May 21 2012. e392.
    [3] Davies BR, Greenwood H, Dudley P, et al. Preclinical Pharmacology of AZD5363, an Inhibitor of AKT: Pharmacodynamics, Antitumor Activity, and Correlation of Monotherapy Activity with Genetic Background. Mol. Cancer Ther. Arp 2012. 11: 873.
- Properties
  - Alternative Name
    
    4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
    
    CAS Number
    
    1143532-39-1
    
    Molecular Formula
    
    C21H25ClN6O2
    
    Molecular Weight
    
    428.92
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥21.45 mg/mL in DMSO; insoluble in H2O; ≥5.04 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Wang C, Bai F, et al. "Estrogen promotes estrogen receptor negative BRCA1-deficient tumor initiation and progression." Breast Cancer Res. 2018 Jul 11;20(1):74. PMID:29996906
    2. Du Q, Zhang S, et al. "Astragaloside IV Inhibits Adipose Lipolysis and Reduces Hepatic Glucose Production via Akt Dependent PDE3B Expression in HFD-Fed Mice." Front Physiol. 2018 Jan 23;9:15. PMID:29410630
    3. Peng T, Dou QP. "Everolimus Inhibits Growth of Gemcitabine-Resistant Pancreatic Cancer Cells via Induction of Caspase-Dependent Apoptosis and G(2) /M Arrest." J Cell Biochem. 2017 Feb 6. PMID:28165150

AZD5363

Background

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