TK216 |
カタログ番号GC38863
One-Click Copy Product Info
|
TK216 は、経口で有効な強力な E26 形質転換特異的 (ETS) 阻害剤です。 TK216 は EWS-FLI1 に直接結合し、EWS-FLI1 タンパク質相互作用を阻害します。 TK216 は、EWS-FLI1 と RNA ヘリカーゼ A の間の結合をブロックします。TK216 には抗がん作用があります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1903783-48-1
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
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].
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
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]
[1]. Spriano F, et al. The ETS Inhibitors YK-4-279 and TK-216 Are Novel Antilymphoma Agents. Clin Cancer Res. 2019 Aug 15;25(16):5167-5176. [2]. Brian Lannutti, et al. Uses of indolinone compounds. US10159660B2.
| Cas No. | 1903783-48-1 | SDF | |
| Canonical SMILES | O=C1NC2=C(C(Cl)=CC=C2Cl)C1(CC(C3=CC=C(C4CC4)C=C3)=O)O | ||
| Formula | C19H15Cl2NO3 | M.Wt | 376.23 |
| 溶解度 | DMSO: ≥ 250 mg/mL (664.49 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6579 mL | 13.2897 mL | 26.5795 mL |
| 5 mM | 531.6 μL | 2.6579 mL | 5.3159 mL |
| 10 mM | 265.8 μL | 1.329 mL | 2.6579 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)