GLPG0634 analogue 是一种 JAK 广谱性抑制剂，对 JAK1/JAK2/JAK3 的IC50值为 50 到 200 nM之间。

GLPG0634 (analog) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.

GLPG0634（p.o.）在大鼠(45%)体内的绝对生物利用度适中,在小鼠(约100%)体内较高.在大鼠和小鼠的CIA模型中,GLPG0634（30 mg/kg/day,大鼠;50 mg/kg,b.i.d.,小鼠）剂量依赖性减少炎症,软骨及骨降解.

在多种细胞系中,GLPG0634抑制IFN-αB2诱导的JAK1/TYK2 Ⅱ型受体信号和IL-2/4诱导的JAK1/JAK3/γc信号（IC50：150-760 nM）。在细胞水平上,GLPG0634对含JAK1的JAK/STAT信号比JAK2激酶的选择性更高。此外,GLPG0634对Th1/Th2/Th17细胞的增殖也有抑制作用。

EC50 values of the test compounds are calculated from serial dilution series ranging from 200 to 0.1 μM. Cells are seeded in 96-well plates at a density of 5,000 cells per well in 100 μL medium. The next day, 100 μL medium containing each test compound is added. Cells are incubated for 16 h, fixed and processed for automated microscopy. EC50 estimates are calculated using four-parameter log-logistic fit with the package drc[1].

1206101-20-3

C23H18N6O2

410.437

GLPG0634 analogue

DMSO:199.8 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years