1. Apoptosis
  2. Apoptosis
  3. TK216

TK216 

Cat. No.: HY-122903 Purity: 99.66%
Handling Instructions

TK216 is a potent E26 transformation specific (ETS) inhibitor. TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity.

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

TK216 Chemical Structure

TK216 Chemical Structure

CAS No. : 1903783-48-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 290 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 990 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

TK216 is a potent E26 transformation specific (ETS) inhibitor[1]. TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity[2].

IC50 & Target

ETS[1]

In Vitro

TK216 (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].
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].

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

TK216 (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
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (664.49 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6579 mL 13.2897 mL 26.5795 mL
5 mM 0.5316 mL 2.6579 mL 5.3159 mL
10 mM 0.2658 mL 1.3290 mL 2.6579 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.53 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.53 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.53 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

TK216TK 216TK-216ApoptosisEWS-FLI1E26,ESTtranscriptionproliferationRNAanticancerEwingsarcomaFriendleukemiavirusInhibitorinhibitorinhibit

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Product name:
TK216
Cat. No.:
HY-122903
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