2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. TK216

TK216 is an orally active and 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

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 121 In-stock
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10 mM * 1 mL in DMSO USD 121 In-stock
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5 mg USD 110 In-stock
10 mg USD 190 In-stock
25 mg USD 380 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of TK216:

TK216 Related Antibodies

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  • Purity & Documentation

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Description

TK216 is an orally active and 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TK216 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

376.23

Formula

C19H15Cl2NO3
CAS No.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (664.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.84%

SDS (393 KB)

COA (257 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6579 mL 13.2897 mL 26.5795 mL 66.4487 mL
5 mM 0.5316 mL 2.6579 mL 5.3159 mL 13.2897 mL
10 mM 0.2658 mL 1.3290 mL 2.6579 mL 6.6449 mL
15 mM 0.1772 mL 0.8860 mL 1.7720 mL 4.4299 mL
20 mM 0.1329 mL 0.6645 mL 1.3290 mL 3.3224 mL
25 mM 0.1063 mL 0.5316 mL 1.0632 mL 2.6579 mL
30 mM 0.0886 mL 0.4430 mL 0.8860 mL 2.2150 mL
40 mM 0.0664 mL 0.3322 mL 0.6645 mL 1.6612 mL
50 mM 0.0532 mL 0.2658 mL 0.5316 mL 1.3290 mL
60 mM 0.0443 mL 0.2215 mL 0.4430 mL 1.1075 mL
80 mM 0.0332 mL 0.1661 mL 0.3322 mL 0.8306 mL
100 mM 0.0266 mL 0.1329 mL 0.2658 mL 0.6645 mL
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TK216 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TK2161903783-48-1TK 216TK-216DNA/RNA SynthesisEWS-FLI1E26ESTtranscriptionproliferationRNAanticancerEwingsarcomaFriendleukemiavirusInhibitorinhibitorinhibit

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