ARRY 520 trifluoroacetate
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 ActivityPotent 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
ARRY-520, a novel KSP inhibitor with potent activity in hematological and taxane-resistant tumor models.
Woessner et al.
Anticancer Res., 2009;29:4373
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.
KSP inhibitor ARRY-520 as a substitute for PacT. in type I ovarian cancer cells.
Kim et al.
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