Filanesib,1781834-99-8

价格询价

品牌MedChemExpress(MCE)
产地美国
货号HY-15187B
更新日期2025年12月05日

MedChemExpress LLC

品牌商

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Filanesib TFA

CAS No. : 1781834-99-8

MCE 国际站：Filanesib TFA

产品活性：Filanesib TFA (ARRY-520 TFA) 是一种选择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 TFA 在体外能诱导自噬导致细胞死亡。Filanesib TFA 具有高效的抗增生活性。

研究领域：Cell Cycle/DNA Damage | Cytoskeleton

作用靶点：Kinesin

In Vitro: 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.
Filanesib TFA induces mitotic arrest in multiple cell lines.
Filanesib TFA exhibits anti-proliferative against a broad range of human and rodent tumor cell lines.
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 .
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.
Filanesib TFA (0.78-6.25 nM; 44 hours) treatment results in G2/M arrest.
Filanesib TFA (10 nM; 16 hours) treatment results in the formation of monopolar spindles.
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.
Filanesib TFA (3 μM; 6-24 hours) is able to induce caspase-2 activation.
Filanesib TFA (0.003-3 μM; 24-48 hours) is cytotoxic in Type II EOC cells.

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