Filanesib(Synonyms: ARRY-520)

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Filanesib (Synonyms: ARRY-520) 纯度: 99.59%

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(Synonyms: ARRY-520)

Filanesib Chemical Structure

CAS No. : 885060-09-3

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Filanesib 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Cytoskeleton Compound Library
  • Anti-Blood Cancer Compound Library
  • Rare Diseases Drug Library

生物活性

Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity[1].

IC50 & Target[1]

KSP

6 nM (IC50)

体外研究
(In Vitro)

Filanesib induces mitotic arrest in multiple cell lines[1].
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[1].
Filanesib (0.001-0.1 nM; 36 hours) induces apoptosis in a dose-dependent manner in HeLa cells[1].
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[1].
Filanesib 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 (3 μM; 6-24 hours) is able to induce caspase-2 activation[3].
Filanesib (0.003-3 μM; 24-48 hours) is cytotoxic in Type II EOC cells[3].

上海金畔生物科技有限公司 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 the formation of nucleosomes and activation of caspases-3 and 7.

Cell Cycle Analysis[1]

Cell Line: HeLa cells
Concentration: 0.78 nM, 1.56 nM, 3.13 nM, 6.25 nM
Incubation Time: 44 hours
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.

体内研究
(In Vivo)

Filanesib (20 mg/kg, 30 mg/kg; i.p.; q4dx3) has anti-tumor activitiy in vivo[3].

上海金畔生物科技有限公司 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.

Clinical Trial

分子量

420.48

Formula

C20H22F2N4O2S
CAS 号

885060-09-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (237.82 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3782 mL 11.8912 mL 23.7823 mL
5 mM 0.4756 mL 2.3782 mL 4.7565 mL
10 mM 0.2378 mL 1.1891 mL 2.3782 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.95 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.95 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.95 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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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