TX1-85-1 是不可逆 HER3 抑制剂，IC50值为 23 nM。它诱导 HER3 蛋白部分降解，并减弱 HER3 依赖性信号传导。它是选择性 HER3 配体，与位于 HER3 的 ATP 结合位点的 Cys721 形成共价键。

TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling. TX1-85-1 is an irreversible Her3 inhibitor (IC50: 23 nM). TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3.

TX1-85-1 has an anti-proliferation (EC50s: 9.9, 11.5, and 16.9 μM for Ovcar8, HCC827 GR6, and PC9 GR4 cells, respectively) [1].

1603845-32-4

C32H36N8O3

580.68

DMSO:3.85 mg/mL (6.63 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years