1. Cell Cycle/DNA Damage
    Cytoskeleton
    Apoptosis
  2. Kinesin
    Apoptosis
  3. Filanesib

Filanesib (Synonyms: ARRY-520)

Cat. No.: HY-15187 Purity: 99.73%
Handling Instructions

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.

For research use only. We do not sell to patients.

Filanesib Chemical Structure

Filanesib Chemical Structure

CAS No. : 885060-09-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 125 In-stock
Estimated Time of Arrival: December 31
5 mg USD 114 In-stock
Estimated Time of Arrival: December 31
10 mg USD 204 In-stock
Estimated Time of Arrival: December 31
50 mg USD 900 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1620 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Filanesib:

Top Publications Citing Use of Products

Publications Citing Use of MCE Filanesib

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

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].

MCE 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.
In Vivo

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

MCE 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
Molecular Weight

420.48

Formula

C₂₀H₂₂F₂N₄O₂S

CAS No.

885060-09-3

SMILES

O=C(N1[[email protected]@](C2=CC=CC=C2)(CCCN)SC(C3=CC(F)=CC=C3F)=N1)N(OC)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (237.82 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

FilanesibARRY-520ARRY520ARRY 520KinesinApoptosiskinesinspindleproteinanti-proliferativeAMLacutemyelocyticleukemiaInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Filanesib
Cat. No.:
HY-15187
Quantity:
MCE Japan Authorized Agent: