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Filanesib

CAS No. : 885060-09-3

MCE 國際站：Filanesib

產(chǎn)品活性：Filanesib (ARRY-520) 是一種選擇性的，非競爭性的紡錘體驅(qū)動蛋白 (KSP) 抑制劑，對人 KSP 作用的 IC₅₀ 值為 6 nM。Filanesib 在體外能通過誘導(dǎo)自噬 (apoptosis) 導(dǎo)致細(xì)胞死亡。Filanesib 具有高效的抗增生活性。

研究領(lǐng)域：Cell Cycle/DNA Damage  |  Cytoskeleton  |  Apoptosis

作用靶點：Kinesin  |  Apoptosis

In Vitro: 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.

In Vivo: Filanesib (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo.

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