TK216 DNA/RNA Synthesis inhibitor

Cat.No.S9718

TK216 is a potent inhibitor targeting E26 transformation specific (ETS) factors via blocking the protein-protein interaction with RNA helicases. This compound exhibits antilymphoma activity.

TK216 DNA/RNA Synthesis inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 376.23

Quality Control

Batch: S971801 DMSO]75 mg/mL]false]Ethanol]50 mg/mL]false]Water]Insoluble]false Purity: 99.96%
99.96

Chemical Information, Storage & Stability

Molecular Weight 376.23 Formula

C19H15Cl2NO3

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1903783-48-1 -- Storage of Stock Solutions

Synonyms ONCT 216, SPH-8216 Smiles OC1(CC(=O)C2=CC=C(C=C2)C3CC3)C(=O)NC4=C(Cl)C=CC(=C14)Cl

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (199.34 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
ETS [1]
In vitro

This compound demonstrates an antitumor activity across several lymphoma cell lines. 

In vivo

TK-216 demonstrates an antitumor activity in vivo. This compound interferes with protein interactions of ETS family members SPIB, in activated B-cell–like type diffuse large B-cell lymphomas, and SPI1, in germinal center B-cell–type diffuse large B-cell lymphomas.[1]

References

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