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K858 (Racemic)

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Catalog No. T3120Cas No. 72926-24-0
Alias K858 Racemic, K858

K858 Racemic (K858) is a selective mitotic kinesin Eg5 inhibitor which acts in an ATP-noncompetitive manner.

K858 (Racemic)

K858 (Racemic)

Copy Product Info
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Catalog No. T3120Alias K858 Racemic, K858Cas No. 72926-24-0
K858 Racemic (K858) is a selective mitotic kinesin Eg5 inhibitor which acts in an ATP-noncompetitive manner.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$39In StockIn Stock
10 mg$64In StockIn Stock
25 mg$129In StockIn Stock
50 mg$213In StockIn Stock
100 mg$326-In Stock
1 mL x 10 mM (in DMSO)$43In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:>99.99%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
K858 Racemic (K858) is a selective mitotic kinesin Eg5 inhibitor which acts in an ATP-noncompetitive manner.
Targets&IC50
EG5:1.3 μM
In vitro
K858 is an ATP-uncompetitive inhibitor of Eg5 that is at least 150-fold more selective for Eg5 than other members of the kinesin superfamily. K858 induces mitotic arrest and growth inhibition through the activation of the Mad2-mediated spindle checkpoint. K858 induces mitotic cell death in Y cells but not in normal cells. K858 induces mitotic arrest, apoptosis, and cell growth inhibition and has no effect on microtubule polymerization.
In vivo
K858 exhibits antitumor activity and induces mitotic arrest in a human tumor xenograft mouse model. K858 exhibits antitumor activity and induces mitotic arrest in human xenograft tumor models. [1]
SynonymsK858 Racemic, K858
Chemical Properties
Molecular Weight277.34
FormulaC13H15N3O2S
Cas No.72926-24-0
SmilesCC(=O)NC1=NN(C(C)=O)C(C)(S1)c1ccccc1
Relative Density.1.27 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 27.7 mg/mL (99.88 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.21 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.6057 mL18.0284 mL36.0568 mL180.2841 mL
5 mM0.7211 mL3.6057 mL7.2114 mL36.0568 mL
10 mM0.3606 mL1.8028 mL3.6057 mL18.0284 mL
20 mM0.1803 mL0.9014 mL1.8028 mL9.0142 mL
50 mM0.0721 mL0.3606 mL0.7211 mL3.6057 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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