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EDO-S101

🥰Excellent
Catalog No. T3516Cas No. 1236199-60-2
Alias Tinostamustine, Minomustine

EDO-S101 (Tinostamustine) is a pan HDAC inhibitor with IC50 values of 9, 9 and 25 nM for HDAC1, HDAC2 and HDAC3 , respectively.

EDO-S101

EDO-S101

🥰Excellent
Purity: 99.44%
Catalog No. T3516Alias Tinostamustine, MinomustineCas No. 1236199-60-2
EDO-S101 (Tinostamustine) is a pan HDAC inhibitor with IC50 values of 9, 9 and 25 nM for HDAC1, HDAC2 and HDAC3 , respectively.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$40In StockIn Stock
2 mg$51In StockIn Stock
5 mg$73In StockIn Stock
10 mg$123In StockIn Stock
25 mg$207In StockIn Stock
50 mg$369In StockIn Stock
1 mL x 10 mM (in DMSO)$70In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Purity:99.44%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
EDO-S101 (Tinostamustine) is a pan HDAC inhibitor with IC50 values of 9, 9 and 25 nM for HDAC1, HDAC2 and HDAC3 , respectively.
Targets&IC50
HDAC1:9nM, HDAC3:25 nM, HDAC2:9nM
In vitro
EDOS101 inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) in a cellular assay by approximately 90% one hour after dosing with 10 mg/kg i.v. HDAC inhibition in PBMCs could not be increased with higher doses up to 50 mg/kg. EDO-S101 triggers apoptosis and shows strong antitumor activity in HL60 and Daudi cells. Initial in vitro experiments in HL60 cells shows an activation of the intrinsic pathway of apoptosis with cleavage of caspases 3, 9 and PARP and a marked reduction of anti-apoptotic proteins XIAP and Mcl-1.
In vivo
Intracellular HDAC inhibition of EDO-S101, which occurs rapidly after dosing is at maximum activity already at the lowest dose of 10 mg/kg and lasts for about 12-16 hours. Exposure to EDO-S101 causes a strong DNA repair response evidenced by activation of pH2AX and p53 in tumors taken from mice bearing subcutaneous human Burkitt's lymphoma. Tumors of BL rapidly shrink or are completely eradicated after i.v. administration of EDO-S101.
Kinase Assay
EDO-S101 is dissolved in DMSO and added to the assay buffer solution. EDO-S101 dilutions of 5 μL of each dilution is added to 50 μL of the reaction mixture including the Fluor de Lys substrate and all of the enzymatic reactions are conducted in duplicate at 37oC for 30 minutes. After enzymatic reactions, 50 μL of 2xHDAC developer is added to each well and fluorescence intensity is measured[1].
SynonymsTinostamustine, Minomustine
Chemical Properties
Molecular Weight415.36
FormulaC19H28Cl2N4O2
Cas No.1236199-60-2
SmilesCN1C=2C(=CC(N(CCCl)CCCl)=CC2)N=C1CCCCCCC(NO)=O
Relative Density.1.27 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature,keep away from direct sunlight | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 30 mg/mL (72.23 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4076 mL12.0378 mL24.0755 mL120.3775 mL
5 mM0.4815 mL2.4076 mL4.8151 mL24.0755 mL
10 mM0.2408 mL1.2038 mL2.4076 mL12.0378 mL
20 mM0.1204 mL0.6019 mL1.2038 mL6.0189 mL
50 mM0.0482 mL0.2408 mL0.4815 mL2.4076 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:
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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

Keywords

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