TK216 [1903783-48-1]
Cat# T13166-5mg
Size : 5mg
Brand : TargetMol
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TK216
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TK216 is a potent inhibitor of E26 transformation-specific (ETS) with anticancer activity.
Cas No. 1903783-48-1
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:97.22%
Appearance:Solid
Color:White
COA HNMR LCMS
Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | TK216 is a potent inhibitor of E26 transformation-specific (ETS) with anticancer activity. |
| In vitro | In DLBCL cell lines, TK216 (500 nM; for 24-72 hours) induces apoptosis [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]. In DLBCL cell lines,TK216 (0.1, 0.3, 1 μM) induces apoptosis , 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]. |
| In vivo | In the TMD-8 xenograft model, TK216 (po; 100 mg/kg; twice daily for 13 days) results in tumor growth inhibition [1]. |
| Molecular Weight | 376.23 |
| Formula | C19H15Cl2NO3 |
| Cas No. | 1903783-48-1 |
| Smiles | OC1(CC(=O)c2ccc(cc2)C2CC2)C(=O)Nc2c1c(Cl)ccc2Cl |
| Relative Density. | 1.473 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 250 mg/mL (664.49 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: < 10 mg/mL (26.58 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (26.58 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||