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Filanesib TFA

Catalog No. T25418   CAS 1781834-99-8
Synonyms: Filanesib trifluoroacetic acid, ARRY-520 TFA, ARRY 520 TFA, ARRY520 TFA

Filanesib (ARRY-520) targets the kinesin spindle protein (KSP) with potential antineoplastic activity. ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during the mitotic phase, and consequently cell death in tumor cells that are actively dividing.

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Filanesib TFA Chemical Structure
Filanesib TFA, CAS 1781834-99-8
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10 mg 35 days $ 788.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Filanesib (ARRY-520) targets the kinesin spindle protein (KSP) with potential antineoplastic activity. ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during the mitotic phase, and consequently cell death in tumor cells that are actively dividing.
Targets&IC50 KSP:6 nM (IC50)
Synonyms Filanesib trifluoroacetic acid, ARRY-520 TFA, ARRY 520 TFA, ARRY520 TFA
Molecular Weight 534.5
Formula C22H23F5N4O4S
CAS No. 1781834-99-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Milic B, Chakraborty A, Han K, Bassik MC, Block SM. KIF15 nanomechanics and kinesin inhibitors, with implications for cancer chemotherapeutics. Proc Natl Acad Sci U S A. 2018 May 15;115(20):E4613-E4622. doi: 10.1073/pnas.1801242115. Epub 2018 Apr 27. PubMed PMID: 29703754; PubMed Central PMCID: PMC5960320. 2. Hernández-García S, San-Segundo L, González-Méndez L, Corchete LA, Misiewicz-Krzeminska I, Martín-Sánchez M, López-Iglesias AA, Algarín EM, Mogollón P, Díaz-Tejedor A, Paíno T, Tunquist B, Mateos MV, Gutiérrez NC, Díaz-Rodriguez E, Garayoa M, Ocio EM. The kinesin spindle protein inhibitor filanesib enhances the activity of pomalidomide and dexamethasone in multiple myeloma. Haematologica. 2017 Dec;102(12):2113-2124. doi: 10.3324/haematol.2017.168666. Epub 2017 Aug 31. PubMed PMID: 28860344; PubMed Central PMCID: PMC5709111. 3. Shah JJ, Kaufman JL, Zonder JA, Cohen AD, Bensinger WI, Hilder BW, Rush SA, Walker DH, Tunquist BJ, Litwiler KS, Ptaszynski M, Orlowski RZ, Lonial S. A Phase 1 and 2 study of Filanesib alone and in combination with low-dose dexamethasone in relapsed/refractory multiple myeloma. Cancer. 2017 Dec 1;123(23):4617-4630. doi: 10.1002/cncr.30892. Epub 2017 Aug 17. PubMed PMID: 28817190; PubMed Central PMCID: PMC5856158. 4. D'Agostino M, Salvini M, Palumbo A, Larocca A, Gay F. Novel investigational drugs active as single agents in multiple myeloma. Expert Opin Investig Drugs. 2017 Jun;26(6):699-711. doi: 10.1080/13543784.2017.1324571. Epub 2017 May 8. Review. PubMed PMID: 28448171.

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Keywords

Filanesib TFA 1781834-99-8 Filanesib trifluoroacetic acid ARRY-520 TFA ARRY 520 TFA ARRY520 TFA inhibitor inhibit

 

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