产品
编 号:F497589
分子式:C20H22F2N4O2S
分子量:420.48
产品类型
结构图
CAS No: 885060-09-3
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产品详情
生物活性:
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.
体内研究:
Filanesib (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo.Animal Model:Female nude mice, EOC mice xenograft model
Dosage:20 mg/kg, 30 mg/kg
Administration:Intraperitoneal injection, q4dx3
Result:Induced a decrease in tumor kinetics in a dose-dependent manner.
体外研究:
Filanesib induces mitotic arrest in multiple cell lines.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.Filanesib (0.001-0.1 nM; 36 hours) induces apoptosis in a dose-dependent manner in HeLa cells.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.Filanesib potently induces cell cycle block and subsequent death in leukemic cells via the mitochondrial pathway and has potential to eradicate AML progenitor cells.Filanesib (3 μM; 6-24 hours) is able to induce caspase-2 activation.Filanesib (0.003-3 μM; 24-48 hours) is cytotoxic in Type II EOC cells.