Name: Dolastatin 10
Price: 669.00 USD

- Overview
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    Background
    
    Dolastatin 10 is an antitumor agent [1].Dolastatin 10 is a potent antimitotic polypeptide isolated from a marine animal and is developed as a potential antitumor agent. Dolastatin 10 is found to have activity to inhibit tubulin polymerization with IC50 value of 1.2μM. Besides that, it potently inhibits vincristine binding to tubulin with a Ki value of 1.4μM in a noncompetitive manner. Dolastatin 10 also shows moderate effect on enhancing the binding of colchicines to tubulin. In addition, Dolastatin 10 has the inhibitory activity in tubulin-dependent GTP binding [1]. In the cellular assay, Dolastatin 10 shows activity against some human leukaemia, lymphoma and solid tumour cell lines (such as OVCAR-3 and NSCLC) with IC50 values ranging from 0.1nM to 10nM. It is currently tested in the clinical trials [2].
    
    [1] Bai R L, Pettit G R, Hamel E. Binding of dolastatin 10 to tubulin at a distinct site for peptide antimitotic agents near the exchangeable nucleotide and vinca alkaloid sites. Journal of Biological Chemistry, 1990, 265(28): 17141-17149.
    [2] Schwartsmann G. Marine organisms and other novel natural sources of new cancer drugs. Annals of Oncology, 2000, 11(suppl 3): 235-243.
- Properties
  - Alternative Name
    
    (2S)-2-[[(2R)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3S,4S)-3-methoxy-1-[(2S)-2-[(1R,2S)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide
    
    CAS Number
    
    110417-88-4
    
    Molecular Formula
    
    C42H68N6O6S
    
    Molecular Weight
    
    785.09
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥78.5 mg/mL in EtOH; insoluble in H2O; ≥67.2 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CCC(C)C(C(CC(=O)N1CCCC1C(C(C)C(=O)NC(CC2=CC=CC=C2)C3=NC=CS3)OC)OC)N(C)C(=O)C(C(C)C)NC(=O)C(C(C)C)N(C)C
    
    * For Research Use Only
- Applications
  - Application Description
    
    Antitumor agent