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

Filanesib (Synonyms: ARRY-520)

製品番号: HY-15187 純度: 99.73%
取扱説明書

Filanesib (ARRY-520) is a selective 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 (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 125 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 114 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 204 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 900 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1620 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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製品説明

Filanesib (ARRY-520) is a selective 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 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 induces mitotic arrest in multiple cell lines[1].
Filanesib 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 (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 (0.78-6.25 nM; 44 hours) treatment results in G2/M arrest[1].
Filanesib (10 nM; 16 hours) treatment results in the formation of monopolar spindles[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 cell death by apoptosis.

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].

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

885060-09-3

SMILES

O=C(N1[[email protected]@](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)

*"≥" 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.
体内:
  • 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.
参考文献
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Keywords:

FilanesibARRY-520ARRY520ARRY 520Kinesinkinesinspindleproteinanti-proliferativeAMLacutemyelocyticleukemiaInhibitorinhibitorinhibit

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製品名:
Filanesib
製品番号:
HY-15187
数量:
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