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Filanesib TFA (Synonyms: ARRY-520 TFA)
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。
Filanesib TFA Chemical Structure
CAS No. : 1781834-99-8
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
Filanesib TFA 的其他形式现货产品:
Filanesib
| 生物活性 |
Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib TFA induces cell death by apoptosis in vitro. Filanesib TFA has potent anti-proliferative activity[1].
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IC50 & Target |
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体外研究
(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[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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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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| Clinical Trial |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[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 Paclitaxel in Type I ovarian cancer cells. J Transl Med. 2009; 7: 63.
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