ARRY 520 trifluoroacetate

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Description: Potent and selective kinesin spindle protein (KSP) inhibitor; induces Mcl-1 degradation
Alternative Names: 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
Purity: ≥98% (HPLC)
Citations (1)
Reviews (1)
Literature (1)

Biological Activity for ARRY 520 trifluoroacetate

ARRY 520 trifluoroacetate is a 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 for ARRY 520 trifluoroacetate

M. Wt 420.48
Formula C20H22F2N4O2S.CF3CO2H
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1781834-99-8
PubChem ID 90488964
Smiles FC1=CC=C(F)C=C1C2=NN(C(N(C)OC)=O)[C@](CCCN)([C@]3=CC=CC=C3)S2.FC(F)(F)C(O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for ARRY 520 trifluoroacetate

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 31.54 75
ethanol 31.54 75

Preparing Stock Solutions for ARRY 520 trifluoroacetate

The following data is based on the product molecular weight 420.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.75 mM 3.17 mL 15.85 mL 31.71 mL
3.75 mM 0.63 mL 3.17 mL 6.34 mL
7.5 mM 0.32 mL 1.59 mL 3.17 mL
37.5 mM 0.06 mL 0.32 mL 0.63 mL

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Product Datasheets for ARRY 520 trifluoroacetate

References for ARRY 520 trifluoroacetate

References are publications that support the biological activity of the product.

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

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 PacT. in type I ovarian cancer cells. J.Transl.Med. 7 63 PMID: 19619321

If you know of a relevant reference for ARRY 520 trifluoroacetate, please let us know.

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1 Citation for ARRY 520 trifluoroacetate

Citations are publications that use Tocris products. Selected citations for ARRY 520 trifluoroacetate include:

Mues et al (2019) High-Complexity shRNA Libraries and PI3 Kinase Inhibition in Cancer: High-Fidelity Synthetic Lethality Predictions. Cell Rep 27 631 PMID: 30970263

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Reviews for ARRY 520 trifluoroacetate

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T-ALL Network and Pharmacological Validation of Synthetic Lethal Screen.
By Anonymous on 03/26/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: T cell line


PMID: 30970263
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Literature in this Area

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Cell Cycle and DNA Damage Research Product Guide

Cell Cycle and DNA Damage Research Product Guide

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