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TK216
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TK216图片
CAS NO:1903783-48-1
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产品介绍
TK216 是一种有效的 E26 转录因子 (ETS) 抑制剂。TK216 直接结合 EWS-FLI1 并抑制 EWS-FLI1 蛋白质相互作用。TK216 可以阻止 EWS-FLI1 与 RNA 解旋酶 A 的结合。TK216 具有抗癌活性。
Cas No.1903783-48-1
Canonical SMILESO=C1NC2=C(C(Cl)=CC=C2Cl)C1(CC(C3=CC=C(C4CC4)C=C3)=O)O
分子式C19H15Cl2NO3
分子量376.23
溶解度DMSO: ≥ 250 mg/mL (664.49 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.