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。
| 生物活性 | Filanesib TFA (ARRY-520 TFA) is a selectivekinesinspindle protein (KSP) inhibitor, with anIC50of 6 nM for human KSP. Filanesib TFA induces cell death byapoptosisin vitro. Filanesib TFA has potent anti-proliferative activity[1]. |
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体外研究
(In Vitro) | Filanesib TFA inhibits human KSP with an IC50of 6 nM by a mechanism demonstrated to be uncompetitive with respect to ATP and noncompetitive with respect to tubulin[1].
Filanesib TFA induces mitotic arrest in multiple cell lines[1].
Filanesib TFA exhibits anti-proliferative against a broad range of human and rodent tumor cell lines[1].
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[1].
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[1].
Filanesib TFA (0.78-6.25 nM; 44 hours) treatment results in G2/M arrest[1].
Filanesib TFA (10 nM; 16 hours) treatment results in the formation of monopolar spindles[1].
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[2].
Filanesib TFA (3 μM; 6-24 hours) is able to induce caspase-2 activation[3].
Filanesib TFA (0.003-3 μM; 24-48 hours) is cytotoxic in Type II EOC cells[3].
Apoptosis Analysis[1] | Cell Line: | Hela cells | | Concentration: | 0.01-0.1 nM | | Incubation Time: | 36 hours | | Result: | Induced cell death by apoptosis. |
Cell Cycle Analysis[1] | Cell Line: | HeLa cells | | Concentration: | 44 hours | | Incubation Time: | 0.78 nM, 1.56 nM, 3.13 nM, 6.25 nM | | Result: | Resulted in G2/M arrest. |
Western Blot Analysis[3] | Cell Line: | Type II EOC cells | | Concentration: | 3 μM | | Incubation Time: | 6 hours, 12 hours, 24 hours | | Result: | Induced caspase-2 activation in a time-dependent manner. |
Cell Cytotoxicity Assay[3] | Cell Line: | Type II EOC cell lines (A2780, CP70, 01-28) | | Concentration: | 0.003 μM, 0.03 μM, 0.3μM, 3 μM | | Incubation Time: | 24 hours, 48 hours | | Result: | Effectively decreased cell viability in a time-dependent manner in the Type II EOC cell lines. |
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体内研究
(In Vivo) | Filanesib TFA (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo[3].
| Animal Model: | Female nude mice, EOC mice xenograft model[3] | | Dosage: | 20 mg/kg, 30 mg/kg | | Administration: | Intraperitoneal injection, q4dx3 | | Result: | Induced a decrease in tumor kinetics in a dose-dependent manner. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
