TK216
Based on 9 publication(s) in Google Scholar
TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.18%
- No. CAS: 1903783-48-1
- Fòrmula: C19H15Cl2NO3
- Peso molecular:376.23
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
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Publications Citing Use of MedChemExpress (MCE) TK216
More- Cancer Res. 2021 Apr 15;81(8):1965-1976. [Abstract]
- Genome Med. 2020 Nov 20;12(1):99. [Abstract]
- Int Immunopharmacol. 2026 Apr 15:175:116408. [Abstract]
- J Cell Mol Med. 2024 Dec;28(23):e70237. [Abstract]
- Genes (Basel). 2023 Oct 8;14(10):1916. [Abstract]
- bioRxiv. 2025 Sep 20.
- Federal University of Rio Grande do Sul. 2025.
- Int J Biol Sci. 2022 Jan 16;18(4):1363-1380. [Abstract]
- bioRxiv. 2020 May.
Ver todos los productos específicos de isoformas DNA/RNA Synthesis
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Actividad biológica
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Helicase |
TK216 (500 nM; for 24-72 hours) induces apoptosis in DLBCL cell lines[1].
TK216 (0.03, 0.06, 0.125, 0.25, 0.5 μM) results in a dose-dependent inhibition of proliferation in Ewing Sarcoma A4573 cell line[1].
TK216 (0.1, 0.3, 1 μM) induces apoptosis in DLBCL cell lines, with the amount of cleaved-Caspase 3 normalized to b-actin and presented as fold over control[1].
TK216 has IC50s of 0.363 μM and 0.152 μM for HL-60 AML cell line and TMD-8 DLBCL cell line[1].
TK216 inhibits EWS-FLI1 (Ewing sarcoma breakpoint region 1/Friend leukemia virus integration 1 fusion protein) protein interactions, leading to a decrease in transcription and proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DLBCL cell lines
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Concentration:500 nM
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Incubation Time:For 24, 48 or 72 hours
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Result:Induced apoptosis in DLBCL cell lines.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-Scid mice subcutaneously inoculated with TMD8 cells[1]
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Dosage:100 mg/kg
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Administration:PO; twice daily for 13 days
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Result:Resulted in tumor growth inhibition.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1903783-48-1
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Appearance Solid
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Peso molecular 376.23
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Fòrmula C19H15Cl2NO3
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Color White to off-white
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SMILES
O=C1NC2=C(C(Cl)=CC=C2Cl)C1(CC(C3=CC=C(C4CC4)C=C3)=O)O
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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 (9)
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Journal Impact Factor
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Most Recent
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Cancer Res
2021 Apr 15;81(8):1965-1976. PMID: 33589517 -
Genome Med
Single cell characterization of B-lymphoid differentiation and leukemic cell states during chemotherapy in ETV6-RUNX1-positive pediatric leukemia identifies drug-targetable transcription factor activities. [Abstract]2020 Nov 20;12(1):99. PMID: 33218352 -
Int Immunopharmacol
ETS1 potentiates pancreatic Pyroptosis in mice with acute pancreatitis by regulating the NKIRAS1/NF-κB Axis. [Abstract]2026 Apr 15:175:116408. PMID: 41722538 -
J Cell Mol Med
Endothelial KDM5B Regulated by Piezo1 Contributes to Disturbed Flow Induced Atherosclerotic Plaque Formation. [Abstract]2024 Dec;28(23):e70237. PMID: 39643939 -
Genes (Basel)
The Small-Molecule E26-Transformation-Specific Inhibitor TK216 Attenuates the Oncogenic Properties of Pediatric Leukemia. [Abstract]2023 Oct 8;14(10):1916. PMID: 37895265 -
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Int J Biol Sci
Cancer-associated adipocytes promote the invasion and metastasis in breast cancer through LIF/CXCLs positive feedback loop. [Abstract]2022 Jan 16;18(4):1363-1380. PMID: 35280694 -
Solvente y solubilidad
DMSO : ≥ 250 mg/mL (664.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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: ≥ 2.08 mg/mL (5.53 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.53 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 (283 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 | 2.6579 mL | 13.2897 mL | 26.5795 mL | 66.4487 mL |
| 5 mM | 0.5316 mL | 2.6579 mL | 5.3159 mL | 13.2897 mL | |
| 10 mM | 0.2658 mL | 1.3290 mL | 2.6579 mL | 6.6449 mL | |
| 15 mM | 0.1772 mL | 0.8860 mL | 1.7720 mL | 4.4299 mL | |
| 20 mM | 0.1329 mL | 0.6645 mL | 1.3290 mL | 3.3224 mL | |
| 25 mM | 0.1063 mL | 0.5316 mL | 1.0632 mL | 2.6579 mL | |
| 30 mM | 0.0886 mL | 0.4430 mL | 0.8860 mL | 2.2150 mL | |
| 40 mM | 0.0664 mL | 0.3322 mL | 0.6645 mL | 1.6612 mL | |
| 50 mM | 0.0532 mL | 0.2658 mL | 0.5316 mL | 1.3290 mL | |
| 60 mM | 0.0443 mL | 0.2215 mL | 0.4430 mL | 1.1075 mL | |
| 80 mM | 0.0332 mL | 0.1661 mL | 0.3322 mL | 0.8306 mL | |
| 100 mM | 0.0266 mL | 0.1329 mL | 0.2658 mL | 0.6645 mL |
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