Name: ELR510444
Price: 289.00 USD

- Overview
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    Background
    
    Microtubules are involved in nucleic and cell organization, division of intracellular structure, and intracellular transport, as well as ciliary and flagellar motility. Microtubule-targeting agents are some of the most effective chemotherapeutic drugs used in the clinic today. ELR510444 is a novel microtubule disruptor with multiple mechanisms of action.In vitro: ELR510444 has potent microtubuledisrupting activity, causing a loss of intracellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells. ELR510444 inhibited cell proliferation, inhibited the rate and extent of purified tubulin assembly potently, and displaced colchicine from tubulin, revealing that the drug directly interacts with tubulin at the colchicine-binding site [1]. In vivo: ELR510444 also shows potent antitumor activity in the MDA-MB-231 xenograft model with at least a 2-fold therapeutic window [1]. Clinical trial: Up to now, ELR510444 is still in the preclinical development stage.
    
    [1] Risinger AL, Westbrook CD, Encinas A, Mülbaier M, Schultes CM, Wawro S, Lewis JD, Janssen B, Giles FJ, Mooberry SL. ELR510444, a novel microtubule disruptor with multiple mechanisms of action. J Pharmacol Exp Ther. 2011 Mar;336(3):652-60.
- Properties
  - Alternative Name
    
    N-(5-(5-cyanothiophen-2-yl)-2-methylphenyl)-4-methylbenzenesulfonamide
    
    CAS Number
    
    1233948-35-0
    
    Molecular Formula
    
    C19H16N2O2S2
    
    Molecular Weight
    
    368.47
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥11.9 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CC1=CC=C(S(NC2=C(C=CC(C3=CC=C(S3)C#N)=C2)C)(=O)=O)C=C1
    
    * For Research Use Only
- Applications
  - Application Description
    
    Novel microtubule disruptor