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

Filanesib  (Synonyms: ARRY-520)

製品番号: HY-15187 純度: 98.23%
COA 取扱説明書

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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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Filanesib 構造式

Filanesib 構造式

CAS 番号 : 885060-09-3

容量 価格（税別） 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 125 在庫あり
Solution
10 mM * 1 mL in DMSO USD 125 在庫あり
Solid
5 mg USD 96 在庫あり
10 mg USD 164 在庫あり
50 mg USD 492 在庫あり
100 mg USD 787 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 5 publication(s) in Google Scholar

Other Forms of Filanesib:

Filanesib 関連抗体

Top Publications Citing Use of Products

Kinesin アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Kinesin-5/Eg5/KSP Kinesin-6 Kinesin-7/CENP-E Kinesin-12 Kinesin-14

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製品説明

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)

体外実験

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.

Filanesib 関連抗体

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.
体内実験

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

MedChemExpress (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.
臨床実験
分子量

420.48

分子式

C20H22F2N4O2S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1[C@@](C2=CC=CC=C2)(CCCN)SC(C3=CC(F)=CC=C3F)=N1)N(OC)C
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.

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
View the 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.

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  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

体内:

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.

  • Protocol 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

    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.
  • Protocol 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

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション

純度: 98.23%

COA (260 KB) LCMS (96 KB)

取扱説明書 (2659 KB)
参考文献

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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Filanesib Related Classifications

  • 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
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Filanesib885060-09-3ARRY-520ARRY520ARRY 520KinesinApoptosiskinesinspindleproteinanti-proliferativeAMLacutemyelocyticleukemiaInhibitorinhibitorinhibit

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製品名:
Filanesib
製品番号:
HY-15187
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