Filanesib (ARRY-520) 是一种选择性的，非竞争性的纺锤体驱动蛋白 (KSP) 抑制剂，对人 KSP 作用的 IC₅₀ 值为 6 nM。Filanesib 在体外能通过诱导自噬 (apoptosis) 导致细胞死亡。Filanesib 具有高效的抗增生活性。

Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC 50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity.

Solid

KSP 6 nM (IC50)

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.

Filanesib (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female nude mice, EOC mice xenograft model

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.
[3]. Ki Hyung Kim, et al. KSP inhibitor ARRY-520 as a substitute for Pacli

In Vitro: DMSO : ≥ 100 mg/mL (237.82 mM)配制储备液