Name: Safingol
Price: 254.00 USD

- Overview
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    Background
    
    Ki: SphK with a Ki of about 5 μmol/LSafingol is a sphingosine and PKC kinases inhibitor.Sphingosine 1-phosphate, a product of sphingosine kinases (SphK), mediates various biological processes including cell proliferation, differentiation, motility, and apoptosis. Protein kinase C (PKC), is a family of protein kinase enzymes involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues.In vitro: Safingol was identified as a potent competitive inhibitor of SphK and had significant in-vitro anticancer activity. Safingol could increase the in-vitro antitumor effect of various chemotherapeutic agents including cisplatin, doxorubicin, and mitomycin C via enhancing chemotherapy induced apoptosis. It was also found that safingol alone induced cell death by autophagy. Safingol was also extensively studied as an inhibitor of PKC, although the Ki was higher than that for SphK [1]. In vivo: Previous studies found that although safingol showed limited single-agent activity in vivo, xenograft experiments had indicated that safingol could increase the antitumor activity of cisplatin without increasing toxicity [1]. Clinical trial: Previous clinical study showed that safingol could be safely administered in combination with cisplatin. As expected from preclinical data, the reversible dose-dependent hepatic toxicity was observed. Target inhibition was achieved with downregulation of S1P. The recommended phase II dose is S 840 mg/m2 and C 60 mg/m2, every 3 weeks [1].
- Properties
  - Alternative Name
    
    L-threo-Dihydrosphingosine,L-threo-Sphinganine; (2S,3S)-2-amino1,3-octadecanediol
    
    CAS Number
    
    15639-50-6
    
    Molecular Formula
    
    C18H39NO2
    
    Molecular Weight
    
    301.5
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤0.25mg/ml in ethanol
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Safingol

Safingol

Background

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