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首页-抗体药物偶连体和PROTACs-PROTAC-TED-690
TED-690

Chemical Structure : TED-690

CAS No.:

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TED-690 (TED690)

货号: PC-26509Not For Human Use, Lab Use Only.

TED-690 is a potent, heterobifunctional TEAD·YAP/TAZ PROTAC degrader, degrades YAP, pYAPS127, and active YAP protein levels with DC50 values of 0.1 μM (Dmax=57%), 0.1 μM (Dmax=80%), and 0.01 uM (Dmax=80%) in MDA-MB-231 cells, also degrades partners YAP and TAZ.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

TED-690 is a potent, heterobifunctional TEAD·YAP/TAZ PROTAC degrader, degrades YAP, pYAPS127, and active YAP protein levels with DC50 values of 0.1 μM (Dmax=57%), 0.1 μM (Dmax=80%), and 0.01 uM (Dmax=80%) in MDA-MB-231 cells, also degrades partners YAP and TAZ.
TED-690 reduced YAP, pYAPS127, and active YAP protein levels, with DC50 values of 0.2 ± 0.2 μM (Dmax = 61%), 0.3 ± 0.3 μM (Dmax = 62%), and 0.03 ± 0.02 μM (Dmax = 61%), respectively, in YAP-amplified small cell lung cancer cell line NCI-H841.
TED-690 degraded pYAPS127 and TEAD with nanomolar DC50 values of 0.03 ± 0.04 μM (Dmax = 70%) and 0.02 ± 0.03 μM (Dmax = 71%), respectively, in triple-negative breast cancer cell line MDA-MB-468.
TED-690 reduced TEAD and TAZ protein levels with DC50 of 0.4 ± 0.1 μM (Dmax = 63%), and TAZ with DC50 of 0.4 ± 0.3 μM (Dmax = 66%) in MDA-MB-468 and TMD-231 cell lines.
TED-690 demonstrated time-dependent degradation, reducing YAP, TEAD, and TAZ protein levels in MDA-MB-231 cells with degradation half-lives of 10.1 ± 1.9 h, 9.6 ± 1.4 h, and 9.7 ± 1.4 h, respectively.
TED-690 inhibited YAP-TEAD transcriptional activity and cell survival.
TED-690 binds to the TEAD lipid pocket have the potential to degrade not only TEAD, but also its binding partners YAP and TAZ.

物理化学性质&存储条件

分子量 788.90
分子式 C42H52N4O11
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-((5-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethoxy)pentyl)oxy)-6-((3-(pentyloxy)phenyl)amino)benzoic acid

参考文献

1. Yeh IJ, et al. ACS Chem Biol. 2026 Apr 8. doi: 10.1021/acschembio.6c00170.

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