Filanesib TFA  (Synonyms: ARRY-520 TFA)

Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC₅₀ of 6 nM for human KSP. Filanesib TFA induces cell death by apoptosis in vitro. Filanesib TFA has potent anti-proliferative activity^[1].

IC50: 6 nM (KSP)^[1]

Filanesib TFA inhibits human KSP with an IC₅₀ of 6 nM by a mechanism demonstrated to be uncompetitive with respect to ATP and noncompetitive with respect to tubulin^[1].
Filanesib TFA induces mitotic arrest in multiple cell lines^[1].
Filanesib TFA exhibits anti-proliferative against a broad range of human and rodent tumor cell lines^[1].
Filanesib TFA (0.001-0.1 nM; 36 hours) induces apoptosis, by a mechanism that is independent of p53 status, as defined by formation of nucleosomes and activation of caspases 3 and 7, as well as accumulation in SubG0/1 by FACS ^[1].
Filanesib TFA (0.1-100 nM; 18 hours) induces the accumulation of phospho-Histone H3 (a marker of mitosis, and an indicator of mitotic arrest) in HeLa cells^[1].
Filanesib TFA (0.78-6.25 nM; 44 hours) treatment results in G2/M arrest^[1].
Filanesib TFA (10 nM; 16 hours) treatment results in the formation of monopolar spindles^[1].
Filanesib TFA potently induces cell cycle block and subsequent death in leukemic cells via the mitochondrial pathway and has potential to eradicate AML progenitor cells^[2].
Filanesib TFA (3 μM; 6-24 hours) is able to induce caspase-2 activation^[3].
Filanesib TFA (0.003-3 μM; 24-48 hours) is cytotoxic in Type II EOC cells^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Filanesib TFA (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

534.50

C₂₂H₂₃F₅N₄O₄S

1781834-99-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Christine Lemieux, et al. ARRY-520, a Novel, Highly Selective KSP Inhibitor with Potent Anti-Proliferative Activity. AACR Annual Meeting. 2007.

  [2]. BZ Carter, et al. Inhibition of KSP by ARRY-520 Induces Cell Cycle Block and Cell Death via the Mitochondrial Pathway in AML Cells.  [Content Brief]

  [3]. Ki Hyung Kim, et al. KSP inhibitor ARRY-520 as a substitute for Paclitaxel in Type I ovarian cancer cells. J Transl Med. 2009; 7: 63.  [Content Brief]