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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
🥰Excellent
Purity: 98.61%
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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $40 | In Stock | |
| 2 mg | $51 | In Stock | |
| 5 mg | $73 | In Stock | |
| 10 mg | $123 | In Stock | |
| 25 mg | $207 | In Stock | |
| 50 mg | $369 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $70 | In Stock |
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CitedSelect Batch
Purity:98.61%
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.Product Introduction
Bioactivity
Chemical Properties
| 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]. |
| Alias | Tinostamustine, Minomustine |
| Molecular Weight | 415.36 |
| Formula | C19H28Cl2N4O2 |
| Cas No. | 1236199-60-2 |
| Smiles | CN1C=2C(=CC(N(CCCl)CCCl)=CC2)N=C1CCCCCCC(NO)=O |
| Relative Density. | 1.27 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 30 mg/mL (72.23 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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