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TK216

🥰Excellent
Catalog No. T13166Cas No. 1903783-48-1

TK216 is a potent inhibitor of E26 transformation-specific (ETS) with anticancer activity.

TK216

TK216

🥰Excellent
Purity: 98.45%
Catalog No. T13166Cas No. 1903783-48-1
TK216 is a potent inhibitor of E26 transformation-specific (ETS) with anticancer activity.
Pack SizePriceAvailabilityQuantity
1 mg$37In Stock
5 mg$89In Stock
10 mg$155In Stock
25 mg$313In Stock
50 mg$538In Stock
100 mg$778In Stock
1 mL x 10 mM (in DMSO)$98In Stock
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Purity:98.45%
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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.
Solubility Information
DMSO: 249 mg/mL (661.83 mM)
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

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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