Molecular Formula | C23H21N7O |
Molar Mass | 411.46 |
Density | 1.45±0.1 g/cm3(Predicted) |
pKa | 12.54±0.40(Predicted) |
Storage Condition | 2-8℃ |
In vitro study | In vitro experiments, GS-9973 in Caco-2 cell monolayer membrane has a good two-way permeability. In cells, GS-9973 is also very selective for Syk, strongly inhibiting BCR-mediated B cell activation and proliferation, as well as immune complex-activated cytokine production in monocytes. The combined use of GS-9973 and idelalisib synergistically inhibited cell survival and disrupted chemokine signaling pathways. In vitro, GS-9973 had good bidirectional permeability in Caco-2 cell monolayer. In cells, GS-9973 is also very selective for Syk, strongly inhibiting BCR-mediated B cell activation and proliferation, as well as immune complex-activated cytokine production in monocytes. The combined use of GS-9973 and idelalisib synergistically inhibited cell survival and disrupted chemokine signaling pathways. |
In vivo study | GS-9973 (1 mg/kg, oral) had moderate to high bioavailability in rats and dogs, respectively. In a rat collagen-induced arthritis model, GS-9973 (1-10 mg/kg, P. O.) significantly inhibited joint inflammation. In addition, GS-9973 also has disease-modifying activity, including inhibition of pannus formation, cartilage damage, bone erosion, tooth formation, etc., with ED50 from 1.2 to 3.9 mg/kg. GS-9973 (1 mg/kg, P. O.) had moderate to high bioavailability in rats and dogs, respectively. In a rat collagen-induced arthritis model, GS-9973 (1-10 mg/kg, P. O.) significantly inhibited joint inflammation. In addition, GS-9973 also has disease-modifying activity, including inhibition of pannus formation, cartilage damage, bone erosion, tooth formation, etc., with ED50 from 1.2 to 3.9 mg/kg. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.43 ml | 12.152 ml | 24.304 ml |
5 mM | 0.486 ml | 2.43 ml | 4.861 ml |
10 mM | 0.243 ml | 1.215 ml | 2.43 ml |
5 mM | 0.049 ml | 0.243 ml | 0.486 ml |