Name: Dolastatin 10 trifluoroacetate
Price: 817.00 USD

- Overview
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    Background
    
    Dolastatin 10 trifluoroacetate is an antitumor agent [1].Dolastatin 10 trifluoroacetate 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 1.2 μM. Besides that, it potently inhibits vincristine binding to tubulin with a Ki value of 1.4 μM 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
    
    2,2,2-trifluoroacetic acid compound with (S,Z)-2-(dimethylamino)-N-((S)-1-(((3R,4S,5S)-1-((S)-2-((1R,2R,Z)-3-hydroxy-1-methoxy-2-methyl-3-(((S)-2-phenyl-1-(thiazol-2-yl)ethyl)imino)propyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxoheptan-4-yl)(methyl)amino)
    
    Molecular Formula
    
    C44H69F3N6O8S
    
    Molecular Weight
    
    899.11
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CC[[email protected]]([[email protected]@](N(C([[email protected]](/N=C(O)/[[email protected]](N(C)C)([H])C(C)C)([H])C(C)C)=O)C)([H])[[email protected]@](OC)([H])CC(N1CCC[[email protected]@]1([H])[[email protected]@](OC)([H])[[email protected]@](/C(O)=N/[[email protected]@](C2=NC=CS2)([H])CC3=CC=CC=C3)([H])C)=O)([H])C.FC(F)(C(O)=O)F
    
    * For Research Use Only
- Applications
  - Application Description
    
    Antitumor agent