TETi76
Based on 1 publication(s) in Google Scholar
TETi76 is an orally active TET family inhibitor with IC50 values ??of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine hydroxymethylation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 97.49%
- No. CAS: 1451750-73-4
- Fòrmula: C10H16O5
- Peso molecular:216.23
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Almacenamiento:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TETi76
More
Customer Validation & Images
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Bio/Physico-chemical Assay
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RT-PCR
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Bio/Physico-chemical Assay
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Flow Cytometry
Actividad biológica
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TET1 1.5 μM (IC50) |
TET2 9.4 μM (IC50) |
TET3 8.8 μM (IC50) |
TETi76 (25 μM; 3 d) induces cell death and inhibits TET dioxygenase activity in SIG-M5 cells[1]. TETi76 (20-37 μM; 12 h) reduces intracellular 5 hmC content in a dose-dependent manner in various human leukemia cell lines (K562, MEG-01, SIG-M5, OCI-AML5, and MOLM13), with the concentration range of 50% inhibition of 5 hmC being 20-37 μM[1].
TETi76 (25 μM; 24 h) mimicks the expression signature caused by TET2 deficiency in gene expression analysis of K562? (TET2 (+/+) and TET2 (-/-) cells, and addition of ascorbic acid, known to enhance TET activity, counteracts the changes induced by TETi76[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TETi76 (25 mg/kg; ip; once daily, 5 days per week; 4 weeks) limits the proliferative advantage of Tet2?/? (CD45.2) cells in the C57BL6 CD45.1 Pep Boy mouse model (lethally irradiated and transplanted with mixed bone marrow cells) without affecting the proportion of mice receiving Tet2+/+ (CD45.2) cells[1].
TETi76 (50 mg/kg; oral) significantly reduces tumor burden in the immunodeficient NSG mouse model (subcutaneously implanted with the human TET2?/? leukemia cell line SIG-M5)[1]).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL6 mice (sex not specified, weight not specified, age not specified) with Tet2+/+, Tet2+/− and Tet2−/− genotypes + Mouse model for observing the effect of TETi76 on spleen size and general health[1]
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Dosage:50 mg/kg
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Administration:Oral administration, 5 days per week, for 3 months
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Result:Did not show significant changes in the overall body weight and overall blood counts of the mice compared with the placebo group.
Decreased the spleen sizes of Tet2-deficient mice in a gene dose-dependent manner.
Chemical Information
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No. CAS 1451750-73-4
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Appearance Liquid
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Peso molecular 216.23
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Fòrmula C10H16O5
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Color Colorless to light yellow
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SMILES
O=C(OCC)C(O)CC(C(OCC)=O)=C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Int J Biol Macromol
Trained immunity driven by Enterococcus faecalis ribosomal protein S11 enhances antigen presentation and boosts influenza vaccine efficacy via nanoparticle delivery. [Abstract]2025 Jun;315(Pt 1):144179. PMID: 40381785
TETi76 purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2025 Jun;315(Pt 1):144179. [Abstract]
TNF-α and NO levels in the supernatants of macrophages treated with TETi76 (25 μM; 24 h) was determined.
TETi76 purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2025 Jun;315(Pt 1):144179. [Abstract]
Relative mRNAs of ribosomal protein genes and expression levels of 18S, 5S, and 28S rRNA in macrophages treated with TETi76 (25 μM; 24 h) were analyzed.
TETi76 purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2025 Jun;315(Pt 1):144179. [Abstract]
Representative polysome profiling of macrophages treated with TETi76 (25 μM; 24 h) was analyzed.
TETi76 purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2025 Jun;315(Pt 1):144179. [Abstract]
Representative flow histogram plots and quantitative analysis of MHC I molecule expression in macrophages treated with TETi76 (25 μM; 24 h).
Solvente y solubilidad
DMSO : 100 mg/mL (462.47 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 (stored under nitrogen). 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 (stored under nitrogen). 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)
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 (11.56 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 (11.56 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Pureza y Documentación
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Ficha de datos (272 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, 6 months; -20°C, 1 month (stored under nitrogen). 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 |
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| DMSO | 1 mM | 4.6247 mL | 23.1235 mL | 46.2471 mL | 115.6176 mL |
| 5 mM | 0.9249 mL | 4.6247 mL | 9.2494 mL | 23.1235 mL | |
| 10 mM | 0.4625 mL | 2.3124 mL | 4.6247 mL | 11.5618 mL | |
| 15 mM | 0.3083 mL | 1.5416 mL | 3.0831 mL | 7.7078 mL | |
| 20 mM | 0.2312 mL | 1.1562 mL | 2.3124 mL | 5.7809 mL | |
| 25 mM | 0.1850 mL | 0.9249 mL | 1.8499 mL | 4.6247 mL | |
| 30 mM | 0.1542 mL | 0.7708 mL | 1.5416 mL | 3.8539 mL | |
| 40 mM | 0.1156 mL | 0.5781 mL | 1.1562 mL | 2.8904 mL | |
| 50 mM | 0.0925 mL | 0.4625 mL | 0.9249 mL | 2.3124 mL | |
| 60 mM | 0.0771 mL | 0.3854 mL | 0.7708 mL | 1.9270 mL | |
| 80 mM | 0.0578 mL | 0.2890 mL | 0.5781 mL | 1.4452 mL | |
| 100 mM | 0.0462 mL | 0.2312 mL | 0.4625 mL | 1.1562 mL |
TETi76 Related Classifications
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