Name: KP372-1
Price: 231.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    IC50: 30-60 nM for thyroid cancer cells
    KP372-1 is a specific Akt inhibitor.
    The phosphatidylinositol 3' kinase (PI3K)/phosphatase, which is a key regulator of cell proliferation and survival, is mutated or activated in various cancers. Akt seems to be a key central node in this pathway and therefore is an promising target.
    In vitro: A previous study found that KP372-1 could block signalling downstream of Akt in thyroid tumour cells, resulting in inhibition of cell proliferation and increased apoptosis [1]. Another study showed that KP372-1 directly inhibited the kinase activity of AKT, FLT3, and PDK1concentration-dependently. Western blot analyses indicated KP372-1 decreased the phosphorylation of AKT on both Ser(473) and Thr(308). Moreover, the treatment of AML cell lines with KP372-1 led to rapid generation of reactive oxygen species and stimulation of oxygen consumption. In addition, KP372-1 was able to induce pronounced apoptosis in AML cell lines and primary samples irrespective of their FLT3 status, but not in normal CD34(+) cells [2].
    In vivo: Up to now, there is no animal in vivo data reported.
    Clinical trial: So far, no clinical study has been conducted.
    
    [1] Mandal, M. ,Kim, S.,Younes, M.N., et al. The Akt inhibitor KP372-1 suppresses Akt activity and cell proliferation and induces apoptosis in thyroid cancer cells. British Journal of Cancer 92(10), 1899-1905 (2005).
    [2] Zeng, Z. ,Samudio, I.J.,Zhang, W., et al. Simultaneous inhibition of PDK1/AKT and Fms-like tyrosine kinase 3 signaling by a small-molecule KP372-1 induces mitochondrial dysfunction and apoptosis in acute myelogenous leukemia. Cancer Research 66(7), 3737-3746 (2006).
- Properties
  - Alternative Name
    
    6H-indeno[1,2-ε]tetrazolo[1,5-b][1,2,4]triazin-6-one, compd. with 10H-indeno[2,1-ε]tetrazolo[1,5-b][1,2,4]triazin-10-one (1:1)
    
    CAS Number
    
    1374996-60-7
    
    Molecular Formula
    
    C10H4N6O·C10H4N6O
    
    Molecular Weight
    
    224.2
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    Purity ≥ 95.00% (sum of isomers)
    
    Solubility
    
    ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

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Background

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