Filanesib

Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC₅₀ of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity^[1]. IC50 & Target: IC50: 6 nM (KSP)^[1] In Vitro: Filanesib induces mitotic arrest in multiple cell lines^[1].
Filanesib exhibits anti-proliferative against a broad range of human and rodent tumor cell lines, including a variety of leukemias and solid tumors, with EC₅₀s between 0.4 nM and 14.4 nM^[1].
Filanesib (0.001-0.1 nM; 36 hours) induces apoptosis in a dose-dependent manner in HeLa cells^[1].
Filanesib (3.13-6.25 nM; 44 hours) causes accumulation of cells in the G2/M phase of the cell cycle in a dose-dependent manner in HeLa cells^[1].
Filanesib 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 (3 μM; 6-24 hours) is able to induce caspase-2 activation^[3].
Filanesib (0.003-3 μM; 24-48 hours) is cytotoxic in Type II EOC cells^[3].
In Vivo: Filanesib (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo^[3].