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CAS No.: 1903783-48-1

TK216 Catalog No. CSN43681

TK-216, an analog of YK-4-279 inhibitor, is a potent and selective EWS-FLI1 inhibitor. TK-216 is in early clinical development for the treatment of Ewing sarcoma.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The ETS family is a diverse group of transcription factors that control the expressions of genes that participate in an array of cellular activities, ranging from mitosis to apoptosis. ^[1]. TK-216 is a first-in-class inhibitor of the ETS-family that is currently in phase 1 trials for patients with relapsed/refractory ES. TK-216 showed potent dose-dependent anti-proliferative activity in most of the cell lines, which comprised ABC-DLBCL (n.=8, median IC50=375 nM), GCB-DLBCL (n.=18, 374 nM), MCL (n.=10,339 nM), MZL (n.=6, 292 nM), CLL (n.=2, 1.1 mM), primary mediastinal large B-cell lymphoma (n=1,547 nM), cutaneous T-cell lymphoma (n=3, 645 nM), PTCL-NOS (n.=1, 436 nM), and ALCL (n.=5, 193nM), and canine DLBCL (n=1, 815 nM). Compared with the control group mice treated with TK-216 (100 mg/kg, BID; p.o.) clearly presented a reduction in tumor grow that day 3 which become much apparent with time (day 5, 8, 11: P<0.01). Mice were treated with TK-216 (100 mg/kg, p.o., q.d. twice a week), lenalidomide (20 mg/kg, i.p., q.d. five days a week) alone or in combination. The combination showed a higher anti-tumor activity compared to control group (P< 0.01 day 22) and to lenalidomide (P<0.01 day 25) or TK-216 (P<0.05 day 29) alone^[2].
参考文献

[1] Sarah Gallant, Gary Gilkeson. ETS transcription factors and regulation of immunity. Arch Immunol Ther Exp (Warsz).May-Jun 2006;54(3):149-63.
[2] Filippo Spriano, Elaine Yee Lin Chung,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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6579 mL
- 13.2896 mL
- 26.5793 mL
- 5 mM
- 0.5316 mL
- 2.6579 mL
- 5.3159 mL
- 10 mM
- 0.2658 mL
- 1.3290 mL
- 2.6579 mL

技术信息

CAS号	1903783-48-1	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C19H15Cl2NO3	运输	蓝冰
分子量	376.23	别名

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TK216 Catalog No. CSN43681

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