Filanesib
Based on 7 publication(s) in Google Scholar
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.
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- Pureza : 99.59%
- No. CAS: 885060-09-3
- Fòrmula: C20H22F2N4O2S
- Peso molecular:420.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Filanesib
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Flow Cytometry
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Apoptosis Analysis
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In Vivo Efficacy Study
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
KSP 6 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.7 nM
Compound: 2; ARRY-520
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Growth inhibition of human HCT116 cells after 72 hrs by MTS assay
Growth inhibition of human HCT116 cells after 72 hrs by MTS assay
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[PMID: 26396688] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Hela cells
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Concentration:0.01-0.1 nM
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Incubation Time:36 hours
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Result:Induced the formation of nucleosomes and activation of caspases-3 and 7.
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Cell Line:HeLa cells
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Concentration:0.78 nM, 1.56 nM, 3.13 nM, 6.25 nM
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Incubation Time:44 hours
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Result:Resulted in G2/M arrest.
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Cell Line:Type II EOC cells
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Concentration:3 μM
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Incubation Time:6 hours, 12 hours, 24 hours
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Result:Induced caspase-2 activation in a time-dependent manner.
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Cell Line:Type II EOC cell lines (A2780, CP70, 01-28)
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Concentration:0.003 μM, 0.03 μM, 0.3μM, 3 μM
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Incubation Time:24 hours , 48 hours
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Result:Effectively decreased cell viability in a time-dependent manner in the Type II EOC cell lines.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice, EOC mice xenograft model[3]
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Dosage:20 mg/kg, 30 mg/kg
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Administration:Intraperitoneal injection, q4dx3
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Result:Induced a decrease in tumor kinetics in a dose-dependent manner.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 885060-09-3
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Appearance Solid
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Peso molecular 420.48
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Fòrmula C20H22F2N4O2S
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Color White to off-white
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SMILES
O=C(N1[C@@](C2=CC=CC=C2)(CCCN)SC(C3=CC(F)=CC=C3F)=N1)N(OC)C
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Synonyms
ARRY-520
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Cell Discov
Single-cell profiling reveals molecular basis of malignant phenotypes and tumor microenvironments in small bowel adenocarcinomas. [Abstract]2022 Sep 14;8(1):92. PMID: 36104333
Filanesib purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 14;8(1):92. [Abstract]
Filanesib (0-100 μM; 36 h) inhibited HUTU-80 cell survival in a dose-dependent manner.
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Cancer Lett
2021 May 28:506:1-10. PMID: 33652084
Filanesib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2021 May 28:506:1-10. [Abstract]
Filanesib (0-10 nM; 48 h) showed antiproliferative effects in the benign meningioma cell line Ben-Men-1 and the anaplastic cell lines NCH93, IOMM-Lee, and KT21-MG cells.
Filanesib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2021 May 28:506:1-10. [Abstract]
Filanesib (10 nM; 24, 48, 72 h) induced cell cycle arrest at G2/M-phase in Ben-Men-1, NCH93, IOMM-Lee, and KT21-MG cells.
Filanesib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2021 May 28:506:1-10. [Abstract]
Filanesib (10 nM; 72 h) induced cell apoptosis in Ben-Men-1, NCH93, IOMM-Lee, and KT21-MG cells.
Filanesib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2021 May 28:506:1-10. [Abstract]
Filanesib (10 mg/kg; i.p.; once every three days on five occasions) inhibited NCH93 tumor growth in NCH93 tumor-bearing mice.
Filanesib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2021 May 28:506:1-10. [Abstract]
Filanesib (10 mg/kg; i.p.; once every three days on five occasions) showed a significant reduction of Ki-67-positive cells in tumor sections.
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NPJ Precis Oncol
Functional screening identifies kinesin spindle protein inhibitor filanesib as a potential treatment option for hepatoblastoma. [Abstract]2025 Apr 25;9(1):122. PMID: 40281281 -
Gene
2025 Jul 5:955:149458. PMID: 40187619 -
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Solvente y solubilidad
In Vitro:
DMSO : ≥ 100 mg/mL (237.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureza y Documentación
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Ficha de datos (303 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3782 mL | 11.8912 mL | 23.7823 mL | 59.4559 mL |
| 5 mM | 0.4756 mL | 2.3782 mL | 4.7565 mL | 11.8912 mL | |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3782 mL | 5.9456 mL | |
| 15 mM | 0.1585 mL | 0.7927 mL | 1.5855 mL | 3.9637 mL | |
| 20 mM | 0.1189 mL | 0.5946 mL | 1.1891 mL | 2.9728 mL | |
| 25 mM | 0.0951 mL | 0.4756 mL | 0.9513 mL | 2.3782 mL | |
| 30 mM | 0.0793 mL | 0.3964 mL | 0.7927 mL | 1.9819 mL | |
| 40 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL | 1.4864 mL | |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4756 mL | 1.1891 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9909 mL | |
| 80 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7432 mL | |
| 100 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5946 mL |
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