Catalog Number: 4676
Chemical Name: (2S)-2-(3-Aminopropyl)-5-(2,5-difluorophenyl)-N-methoxy-N-methyl-2-phenyl-1,3,4-thiadiazole-3(2H)-carboxamide trifluoroacetate
Biological Activity
Potent kinesin spindle protein (KSP) inhibitor (IC50 = 6 nM); selective for KSP over >250 other receptors and kinases at a concentration of 10 μM. Displays robust antitumor activity in bortezomib-resistant xenografts either alone or in combination with bortezomib. Induces degradation of Mcl-1; exhibits comparable cytotoxic activity to taxol (Cat. No. 1097) in epithelial ovarian cancer cells. Active in vivo.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 75 mM in DMSO and to 75 mM in ethanol
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. KSP inhibitor ARRY-520 as a substitute for Paclitaxel in type I ovarian cancer cells.
    Kim et al.
    J.Transl.Med., 2009;7:63
  2. ARRY-520, a novel KSP inhibitor with potent activity in hematological and taxane-resistant tumor models.
    Woessner et al.
    Anticancer Res., 2009;29:4373
  3. Mcl-1 stability determines mitotic cell fate of human multiple myeloma tumor cells treated with the kinesin spindle protein inhibitor ARRY-520.
    Tunquist et al.
    Mol.Cancer.Ther., 2010;9:2046
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