Decernotinib

JAK3:2.5 nM(Ki)

在大鼠胶原诱导性关节炎模型中，Decernotinib(50 mg/kg, 口服) 显示出剂量依赖性地减少踝部肿胀和爪重，并改善爪部组织病理学评分。在小鼠草酰胺诱导的迟发型超敏反应模型中，Decernotinib(50 mg/kg, 口服) 显著抑制耳部水肿。[1] 在大鼠HvG模型中，Decernotinib(50 mg/kg, 口服) 以剂量依赖的方式抑制腘淋巴结 (PLN) 增生。[2]

在HT-2细胞中，Decernotinib抑制了IL-2刺激的HT-2 STAT-5磷酸化、人类T细胞爆发增殖和CD40L/IL-4诱导的B细胞增殖。[1]

Ethanol:16 mg/mL (40.78 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:72 mg/mL (183.5 mM)

Frozen purified human B cells atr thawed, washed, and resuspended in complete medium. Cells are plated onto a 96-well plate at a density of 2 × 105 cells/well. VX-509 is added, and plates are incubated for 30 minutes at 37°C, followed by stimulation with a combination of 10 ng/ml IL-4 and 1 μg/ml CD40L. DMSO alone is added to the top two rows, one of which is stimulated with IL-4 or CD40L (negative control) and the other of which served as a proliferation control. The plates are incubated at 37°C for 6 days. On day 6, cells are pulsed with [3H]thymidine for 7 hours and harvested onto filters for radioactive determination using a PerkinElmer-Wallace beta counter (1205 Betaplate Beta Liquid Scintillation Counter). Data are analyzed with Softmax pro software to generate an IC50 value.(Only for Reference)