Tinostamustine
Based on 4 publication(s) in Google Scholar
Tinostamustine (EDO-S101) is a pan HDAC inhibitor; inhibits HDAC6, HDAC1, HDAC2 and HDAC3 with IC50 values of 6 nM, 9 nM, 9 nM and 25 nM, respectively.
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- Pureza: 99.64%
- No. CAS: 1236199-60-2
- Fòrmula: C19H28Cl2N4O2
- Peso molecular:415.36
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tinostamustine
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Actividad biológica
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HDAC6 6 nM (IC50) |
HDAC1 9 nM (IC50) |
HDAC2 9 nM (IC50) |
HDAC3 25 nM (IC50) |
HDAC10 72 nM (IC50) |
HDAC8 107 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Kasumi 1 | IC50 |
820 nM
Compound: 22
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Cytotoxicity against human Kasumi 1 cells assessed as inhibition of cell growth by MTT assay
Cytotoxicity against human Kasumi 1 cells assessed as inhibition of cell growth by MTT assay
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[PMID: 32791404] |
| MEF | IC50 |
5700 nM
Compound: 9
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Antiproliferative activity against mouse MEF cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against mouse MEF cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
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[PMID: 37989059] |
| NB-4 | IC50 |
900 nM
Compound: 22
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Cytotoxicity against human NB-4 cells assessed as inhibition of cell growth by MTT assay
Cytotoxicity against human NB-4 cells assessed as inhibition of cell growth by MTT assay
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[PMID: 32791404] |
| NCI-H460 | IC50 |
2200 nM
Compound: 9
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Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay
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[PMID: 37989059] |
| Panel NCI-60 (60 carcinoma cell lines) | IC50 |
2.2 μM
Compound: 162
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Cytotoxicity against human Panel NCI-60 (60 carcinoma cell lines)
Cytotoxicity against human Panel NCI-60 (60 carcinoma cell lines)
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[PMID: 33077264] |
Tinostamustine inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) in a cellular assay by approximately 90% one hour after dosing with 10mg/kg i.v. HDAC inhibition in PBMCs could not be increased with higher doses up to 50mg/kg. Tinostamustine 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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1236199-60-2
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Appearance Solid
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Peso molecular 415.36
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Fòrmula C19H28Cl2N4O2
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Color White to off-white
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SMILES
O=C(NO)CCCCCCC1=NC2=CC(N(CCCl)CCCl)=CC=C2N1C
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Synonyms
EDO-S101; NL-101
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Nutrients
Butyrate Protects Barrier Integrity and Suppresses Immune Activation in a Caco-2/PBMC Co-Culture Model While HDAC Inhibition Mimics Butyrate in Restoring Cytokine-Induced Barrier Disruption. [Abstract]2023 Jun 15;15(12):2760. PMID: 37375664 -
Int J Mol Sci
Tinostamustine (EDO-S101) and Its Combination with Celecoxib or Temozolomide as a Therapeutic Option for Adult-Type Diffuse Gliomas. [Abstract]2025 Jan 14;26(2):661. PMID: 39859375 -
Int J Mol Sci
Butyrate Prevents Induction of CXCL10 and Non-Canonical IRF9 Expression by Activated Human Intestinal Epithelial Cells via HDAC Inhibition. [Abstract]2022 Apr 2;23(7):3980. PMID: 35409339
Solvente y solubilidad
DMSO : 100 mg/mL (240.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.02 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
Tinostamustine is dissolved in DMSO and added to the assay buffer solution. Tinostamustine 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 37°C for 30 minutes. After enzymatic reactions, 50 μL of 2xHDAC developer is added to each well and fluorescence intensity is measured[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats: The duration of HDAC inhibition is assessed in 12 female rats after receiving a single dose of either vehicle or Tinostamustine (25mg/kg). Blood samples from EDO-S101 treated rats are collected 1hr, 3hr, 6hr, 16hr and 24hr post dosing (n=2 per time point). Blood sample from vehicle treated rats (n=2) are collected 24hr post dosing[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.4076 mL | 12.0378 mL | 24.0755 mL | 60.1888 mL |
| 5 mM | 0.4815 mL | 2.4076 mL | 4.8151 mL | 12.0378 mL | |
| 10 mM | 0.2408 mL | 1.2038 mL | 2.4076 mL | 6.0189 mL | |
| 15 mM | 0.1605 mL | 0.8025 mL | 1.6050 mL | 4.0126 mL | |
| 20 mM | 0.1204 mL | 0.6019 mL | 1.2038 mL | 3.0094 mL | |
| 25 mM | 0.0963 mL | 0.4815 mL | 0.9630 mL | 2.4076 mL | |
| 30 mM | 0.0803 mL | 0.4013 mL | 0.8025 mL | 2.0063 mL | |
| 40 mM | 0.0602 mL | 0.3009 mL | 0.6019 mL | 1.5047 mL | |
| 50 mM | 0.0482 mL | 0.2408 mL | 0.4815 mL | 1.2038 mL | |
| 60 mM | 0.0401 mL | 0.2006 mL | 0.4013 mL | 1.0031 mL | |
| 80 mM | 0.0301 mL | 0.1505 mL | 0.3009 mL | 0.7524 mL | |
| 100 mM | 0.0241 mL | 0.1204 mL | 0.2408 mL | 0.6019 mL |
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