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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
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
TK216 是一种口服有效的 E26 转录因子抑制剂,具有抗癌活性。它直接结合 EWS-FLI1 并抑制 EWS-FLI1 蛋白质相互作用,也可阻止 EWS-FLI1 与 RNA 解旋酶 A 的结合。

产品描述

TK216 is a potent inhibitor of E26 transformation-specific (ETS) with anticancer activity.

体外活性

In DLBCL cell lines, TK216 (500 nM; for 24-72 hours) induces apoptosis [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]. In DLBCL cell lines,TK216 (0.1, 0.3, 1 μM) induces apoptosis , 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].

体内活性

In the TMD-8 xenograft model, TK216 (po; 100 mg/kg; twice daily for 13 days) results in tumor growth inhibition [1].

Cas No.

1903783-48-1

分子式

C19H15Cl2NO3

分子量

376.23

储存和溶解度

DMSO:249 mg/mL(661.83 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years