ARRY 520 trifluoroacetate

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Cat.No. 4676 - ARRY 520 trifluoroacetate | C20H22F2N4O2S.CF3CO2H | CAS No. 1781834-99-8
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)
Datasheet
Citations (1)
Reviews
Literature (1)

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 420.48
Formula C20H22F2N4O2S.CF3CO2H
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1781834-99-8
PubChem ID 90488964
InChI Key CIJUJPVFECBUKG-BDQAORGHSA-N
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

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

Preparing Stock Solutions

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.

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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References

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


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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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Literature in this Area

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Cancer

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