Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor TK216 For research use only.

TK216

Synonyms: ONCT 216, SPH-8216

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

TK216 Chemical Structure

TK216 Chemical Structure

CAS: 1903783-48-1

Selleck's TK216 has been cited by 1 publication

Purity & Quality Control

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

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Biological Activity

Description

TK216 is a potent inhibitor targeting E26 transformation specific (ETS) factors via blocking the protein-protein interaction with RNA helicases. TK216 exhibits antilymphoma activity.
Targets
ETS [1]
In vitro
In vitro

TK-216 demonstrates an antitumor activity across several lymphoma cell lines. Synergistic activity is observed when TK-216 is combined with the BCL2 inhibitor venetoclax and with the immunomodulatory drug lenalidomide.[1]
Cell Research Cell lines ABC-DLBCL, GCB-DLBCL, MCL, MZL, CLL, primary mediastinal large B-cell lymphoma, cutaneous T-cell lymphoma, PTCL-NOS, ALCL, canine DLBCL
Concentrations 50 nM
Incubation Time 24 h, 48 h, 72 h
Method

For TK-216, cell lines are seeded in 384-well plates at the density of 2,000 cells/well using the VIAFLO 96/384 hand-held electronic channel pipette and then treated with D300e Digital Dispenser. Cell lines are either untreated or treated with TK-216 at 500 nmol/L accompanied by DMSO as solvent control for 24, 48, and 72 hours.
In Vivo
In vivo

TK-216 demonstrates an antitumor activity in vivo. TK-216 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]
Animal Research Animal Models NOD-Scid (NOD.CB17-Prkdcscid/NCrHsd) mice
Dosages 100 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 376.23 Formula

C19H15Cl2NO3
CAS No. 1903783-48-1 SDF --
Smiles OC1(CC(=O)C2=CC=C(C=C2)C3CC3)C(=O)NC4=C(Cl)C=CC(=C14)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 75 mg/mL ( (199.34 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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