ARRY 520 trifluoroacetate

Cat. No. 4676

ARRY 520 trifluoroacetate C20H22F2N4O2S.CF3CO2H [885060-09-3]

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Alternative Name: Filanesib

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

Soluble to 75 mM in DMSO and to 75 mM in ethanol
>98 %
Store at -20°C

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Tunquist et al (2010) Mcl-1 stability determines mitotic cell fate of human multiple myeloma tumor cells treated with the kinesin spindle protein inhibitor ARRY-520. Mol.Cancer.Ther. 9 2046. PMID: 20571074.

Kim et al (2009) KSP inhibitor ARRY-520 as a substitute for Paclitaxel in type I ovarian cancer cells. J.Transl.Med. 7 63. PMID: 19619321.

Woessner et al (2009) ARRY-520, a novel KSP inhibitor with potent activity in hematological and taxane-resistant tumor models. Anticancer Res. 29 4373. PMID: 20032381.

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