TK216 是一种口服有效的 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。

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.

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ETS

TK216 (500 nM; for 24-72 hours) induces apoptosis in DLBCL cell lines.
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.
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.
TK216 has IC50s of 0.363 μM and 0.152 μM for HL-60 AML cell line and TMD-8 DLBCL cell line.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

TK216 (po; 100 mg/kg; twice daily for 13 days) results in tumor growth inhibition of the TMD-8 xenograft model.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NOD-Scid mice subc

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Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 250 mg/mL (664.49 mM)配制储备液