TK216 [1903783-48-1]

Référence T13166-5mg

Conditionnement : 5mg

Marque : TargetMol

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TK216

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TK216 is a potent inhibitor of E26 transformation-specific (ETS) with anticancer activity.
TK216
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
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].
Chemical Properties
Molecular Weight376.23
FormulaC19H15Cl2NO3
Cas No.1903783-48-1
SmilesOC1(CC(=O)c2ccc(cc2)C2CC2)C(=O)Nc2c1c(Cl)ccc2Cl
Relative Density.1.473 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.6579 mL13.2897 mL26.5795 mL132.8974 mL
5 mM0.5316 mL2.6579 mL5.3159 mL26.5795 mL
10 mM0.2658 mL1.3290 mL2.6579 mL13.2897 mL
20 mM0.1329 mL0.6645 mL1.3290 mL6.6449 mL
50 mM0.0532 mL0.2658 mL0.5316 mL2.6579 mL
100 mM0.0266 mL0.1329 mL0.2658 mL1.3290 mL
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.

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