CNX774 是一种选择性的、具有口服活性的、不可逆的BTK抑制剂 (IC50<1 nM)。它能够特异性靶向 BTK 的 Cys 481进行共价修饰。

CNX-774 is a highly specific, irreversible, and orally active BTK inhibitor (IC50<1 nM).

在细胞试验中,CNX-774以BTK的ATP结合位点Cys-481残基为靶点从而抑制其活性（IC50：1-10 nM）。

In vitro kinase assays: The p38α and p38β are assayed in 25 mM Tris-HCl, pH 7.5, containing 0.1 mM EGTA, with myelin basic protein (0.33 mg/mL) as substrate. Assays are performed either manually for 10 minutes at 30 °C in 50 μL incubations using [γ-33P]ATP, or with a Biomek 2000 Laboratory Automation Workstation in a 96-well format for 40 minutes at ambient temperature in 25 μL incubations using [γ-33P]ATP. The concentrations of ATP and magnesium acetate are 0.1 mM and 10 mM respectively. All assays are initiated with MgATP. Manual assays are terminated by spotting aliquots of incubation on to phosphocellulose paper, followed by immersion in 50 mM phosphoric acid. Robotic assays are terminated by the addition of 5 μL of 0.5 M phosphoric acid before spotting aliquots on to P30 filter mats. All papers are then washed four times in 50 mM phosphoric acid to remove ATP, once in acetone (manual incubations) or methanol (robotic incubations), and then dried and counted for radioactivity.

1202759-32-7

C26H22FN7O3

499.506

CNX 774

H2O:<1 mgml
DMSO:93 mg/mL (186.2 mM)
Ethanol:2 mg/mL (4.0 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years