1. Apoptosis
  2. Apoptosis
  3. TK216

TK216 

Cat. No.: HY-122903
Handling Instructions

TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions, leading to a decrease in transcription and proliferation. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 is active in oncogenesis and inhibits apoptosis.

For research use only. We do not sell to patients.

TK216 Chemical Structure

TK216 Chemical Structure

CAS No. : 1903783-48-1

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Description

TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions, leading to a decrease in transcription and proliferation. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 is active in oncogenesis and inhibits apoptosis[1].

IC50 & Target

EWS-FLI1 protein[1]

In Vitro

TK-216 (500 nM; for 24-72 hours) induces apoptosis in DLBCL cell lines[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].
TK216 (0.1, 0.3, 1 μM) induces apoptosis in DLBCL cell lines, with the amount of cleaved-Caspase 3 normalized to b-actin and presented as fold over control[1].
TK-216 has IC50s of 0.363 μM and 0.152 μM for HL-60 AML cell line and TMD-8 DLBCL cell line[1].

Apoptosis Analysis[1]

Cell Line: DLBCL cell lines
Concentration: 500 nM
Incubation Time: For 24, 48 or 72 hours
Result: Induced apoptosis in DLBCL cell lines.
In Vivo

TK-216 (po; 100 mg/kg; twice daily for 13 days) results in tumor growth inhibition of the TMD-8 xenograft model[1].

Animal Model: NOD-Scid mice subcutaneously inoculated with TMD8 cells[1]
Dosage: 100 mg/kg
Administration: Po; twice daily for 13 days
Result: Resulted in tumor growth inhibition.
Molecular Weight

376.23

Formula

C₁₉H₁₅Cl₂NO₃

CAS No.

1903783-48-1

SMILES

O=C1NC2=C(C(Cl)=CC=C2Cl)C1(CC(C3=CC=C(C4CC4)C=C3)=O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

TK216TK 216TK-216ApoptosisInhibitorinhibitorinhibit

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TK216
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