Tefinostat
Based on 1 publication(s) in Google Scholar
Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.65%
- No. CAS: 914382-60-8
- Fòrmula: C28H37N3O5
- Peso molecular:495.61
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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) Tefinostat
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
HDAC |
In Vitro
Tefinostat (CHR-2845) (1-4 nM) has efficacy in AML cell lines HL60 (M2 FAB type), MV411 (M4, FLT3-ITD), OCIAML3 (M4 NPM1mut) and THP1 (M5) with EC50 values of 2.3 μM, 57 nM, 110 nM and 560 nM, respectively[1].
Tefinostat (0, 0.5, 1 and 5μM; 24, 48 h) has dose-dependent induction of apoptosis and significant growth inhibitory effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:AML cell lines
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Concentration:1-4 nM
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Incubation Time:
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Result:Had significant growth inhibitory effects.
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Cell Line:myelo-monocytic cell lines and HL60 cells
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Concentration:0, 0.5, 1 and 5μM
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Incubation Time:24, 48 h
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Result:Showed strong apoptotic induction in myelo-monocytic cell lines THP1, MV411 (FLT3-ITD) and OCIAML3 within 24 hours and only reached in nonmonocytic HL60 cells at much higher concentrations.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 914382-60-8
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Appearance Solid
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Peso molecular 495.61
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Fòrmula C28H37N3O5
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Color White to off-white
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SMILES
O=C(OC1CCCC1)[C@H](C2=CC=CC=C2)NCC3=CC=C(NC(CCCCCCC(NO)=O)=O)C=C3
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Synonyms
CHR-2845
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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 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Biomolecules
Efficacy of HDAC Inhibitors in Driving Peroxisomal β-Oxidation and Immune Responses in Human Macrophages: Implications for Neuroinflammatory Disorders. [Abstract]2023 Nov 23;13(12):1696. PMID: 38136568
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (201.77 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (5.04 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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
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Phagocytosis Functional Assay
A phagocytosis functional assay measures the ability of phagocytic cells, such as neutrophils, macrophages, monocytes, or microglia/macrophages, to bind and internalize particulate targets including bacteria, yeast particles, beads, or myelin particles. Fluorescent flow-cytometry assays detect target uptake as fluorescence associated with gated phagocytes, while pH-sensitive dyes such as pHrodo increase signal in acidic phagosomal compartments and therefore preferentially report internalized particles rather than particles remaining outside the cell. Microscopy or high-content imaging can be used to confirm intracellular localization and, in some protocols, to follow uptake kinetics.
Pureza y Documentación
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Ficha de datos (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0177 mL | 10.0886 mL | 20.1772 mL | 50.4429 mL |
| 5 mM | 0.4035 mL | 2.0177 mL | 4.0354 mL | 10.0886 mL | |
| 10 mM | 0.2018 mL | 1.0089 mL | 2.0177 mL | 5.0443 mL | |
| 15 mM | 0.1345 mL | 0.6726 mL | 1.3451 mL | 3.3629 mL | |
| 20 mM | 0.1009 mL | 0.5044 mL | 1.0089 mL | 2.5221 mL | |
| 25 mM | 0.0807 mL | 0.4035 mL | 0.8071 mL | 2.0177 mL | |
| 30 mM | 0.0673 mL | 0.3363 mL | 0.6726 mL | 1.6814 mL | |
| 40 mM | 0.0504 mL | 0.2522 mL | 0.5044 mL | 1.2611 mL | |
| 50 mM | 0.0404 mL | 0.2018 mL | 0.4035 mL | 1.0089 mL | |
| 60 mM | 0.0336 mL | 0.1681 mL | 0.3363 mL | 0.8407 mL | |
| 80 mM | 0.0252 mL | 0.1261 mL | 0.2522 mL | 0.6305 mL | |
| 100 mM | 0.0202 mL | 0.1009 mL | 0.2018 mL | 0.5044 mL |
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