TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC 50 of 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 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.
性状
Solid
IC50 & Target[1][2]
ErbB3 23 nM (IC50)
体外研究(In Vitro)
TX1-85-1 possesses an anti-proliferation EC50s of 9.9, 11.5, and 16.9 μM for Ovcar8, HCC827 GR6, and PC9 GR4 cells, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Xie T, et al. Pharmacological targeting of the pseudokinase Her3. Nat Chem Biol. 2014 Dec;10(12):1006-12.
溶解度数据
In Vitro: DMSO : 3.85 mg/mL (6.63 mM; Need ultrasonic)配制储备液